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ANASTROZOLE
Anastrozole available under trade name of Arimidex, AstraZeneca is a drug used to treat breast cancer after surgery and for metastases in post-menopausal women.
Anastrozole is an aromatase inhibitor which interrupts a critical step in the body's synthesis of estrogen. Some breast cancer cells require estrogen to grow and eliminating estrogen suppresses their growth.
AREDIA
Aredia has been approved for treatment of osteolytic bone metastases of breast cancer, in conjunction with standard antineoplastic therapy.
Aredia is the first drug that has been proven to reduce the incidence of skeletal complications of metastatic breast cancer, thereby reducing the need for radiation therapy or surgery to the bone.
It has also been shown to provide relief of bone pain caused by metastatic breast cancer, thereby reducing the need for narcotic analgesics.
ARIMIDEX
Arimidex has been approved as a treatment for advanced breast cancer in postmenopausal women whose disease has progressed following therapy with tamoxifen.
The FDA made its decision after evaluating results of clinical studies involving more than 750 subjects. Results from the two studies showed that Arimidex is effective in the treatment of advanced breast cancer.
AVASTIN
In 2004 approved by FDA as a first-line treatment of patients with metastatic carcinoma of the colon and rectum (in combination with intravenous 5-fluorouracil-based chemotherapy).
In 2006 approved by FDA as a first-line treatment of patients with locally advanced, metastatic or recurrent non-small cell lung cancer in combination with platinum-based chemotherapy.
In February 2008, the FDA approved Avastin for use with chemotherapy to treat certain cases of advanced breast cancer.
In 2009 the FDA has approved the drug Avastin to treat a type of brain cancer called glioblastoma that progresses despite treatment with other therapies.
AVEMAR
Avemar is a complex of multiple biologically active molecules obtained from fermented wheat germ extract. Preclinical studies suggest Avemar has potential activity in stimulating the immune system.
BEVACIZUMAB
Bevacizumab available under trade name of Avastin, Genentech/Roche is a humanized monoclonal antibody that recognises and blocks vascular endothelial growth factor. Bevacizumab is currently approved by the U.S. Food and Drug Administration (FDA) for cancers that are metastatic (have spread to other parts of the body). It received its first approval in 2004 was for combination use with standard chemotherapy for metastatic colon cancer and non-small cell lung cancer.
Clinical studies are underway in non-metastatic breast cancer, renal cell carcinoma, glioblastoma multiforme, ovarian cancer, castrate-resistant (formally called hormone refractory) prostate cancer, non-metastatic unresectable liver cancer and metastatic or unresectable locally advanced pancreatic cancer.
BICALUTAMIDE
Bicalutamide marketed by AstraZeneca with the brand names Casodex and Cosudex is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.
Bicalutamide acts as a pure anti-androgen by binding to the androgen receptor(AR) and preventing the activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones.
It was first launched in 1995 as a combination treatment (with surgical or medical castration) for advanced prostate cancer and subsequently launched as monotherapy for the treatment of earlier stages of the disease.
BORTEZOMIB
Bortezomib marketed as Velcade by Millennium Pharmaceuticals is the first therapeutic proteasome inhibitor to be tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma.In multiple myeloma, complete clinical responses have been obtained in patients with otherwise refractory or rapidly advancing disease.
Bortezomib is a medication which interferes with the growth of cancer cells and restricts them from spreading in the body.This medication taken along with antifungal drugs (clotrimazole, itraconazole), antidepressant drugs(nefazodone, paroxetine) or barbiturate (amobarbital, butabarbital) may effect its performance.
The mechanism of action of bortezomib combination therapy with activation of PKC-d can enhance the therapeutic effect of bortezomib providing a unique opportunity to overcome resistance to conventional chemotherapy.
CAMPTO
Campto is a cancer medication that interferes with the growth of cancer cells and slows their growth and spread in the body. Campto is used to treat cancers of the colon and rectum.
It is usually given with other cancer medicines in a combination chemotherapy.
CAMPTOSAR
Irinotecan available under brand name of Camptosar is a drug used for the treatment of cancer.
Irinotecan is a topoisomerase 1 inhibitor which prevents DNA from unwinding. Chemically, it is a semisynthetic analogue of the natural alkaloid camptothecin.
Its main use is in colon cancer, particularly in combination with other chemotherapy agents. This includes the regimen FOLFIRI which consists of infusional 5-fluorouracil, leucovorin, and irinotecan.
Irinotecan was approved by the U.S. Food and Drug Administration (FDA) in 1994. During development, it was known as CPT-11.
CAPECITABINE
Capecitabine available under brand name ofXeloda is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers. Capecitabine is a prodrug that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue.
In the UK, capecitabine is approved by the National Institute for Health and Clinical Excellence (NICE) for colon and colorectal cancer and locally advanced or metastatic breast cancer.
CASODEX
Casodex is an anti-androgen. It works in the body by preventing the actions of androgens (male hormones).
Casodex is used together with another hormone to treat prostate cancer.
CETUXIMAB
Cetuximab is a chimeric (mouse/human) monoclonal antibody, an epidermal growth factor receptor (EGFR) inhibitor, given by intravenous infusion for treatment of metastatic colorectal cancer and head and neck cancer.
DOCETAXEL
Taxotere® (docetaxel) Injection Concentrate Indications:
Breast Cancer
TAXOTERE® is indicated for the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy
TAXOTERE® in combination with doxorubicin and cyclophosphamide is indicated for the adjuvant treatment of patients with operable node-positive breast cancer
Non-Small Cell Lung Cancer
TAXOTERE®, as a single agent, is indicated for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) after failure of prior platinum-based chemotherapy
TAXOTERE® in combination with cisplatin is indicated for the treatment of patients with unresectable, locally advanced or metastatic NSCLC who have not previously received chemotherapy for this condition.
Prostate Cancer
TAXOTERE® in combination with prednisone is indicated for the treatment of patients with androgen independent (hormone refractory) metastatic prostate cancer.
Gastric Cancer
TAXOTERE® in combination with cisplatin and fluorouracil is indicated for the treatment of patients with advanced gastric adenocarcinoma, including adenocarcinoma of the gastroesophageal junction, who have not received prior chemotherapy for advanced disease.
Head and Neck Cancer
TAXOTERE® in combination with cisplatin and fluorouracil is indicated for the induction treatment of patients with locally advanced squamous cell carcinoma of the head and neck (SCCHN).
ELOXATIN
Eloxatin, administered as an injection in combination with infusional 5-fluorouracil (5-FU) and leucovorin (LV), is indicated for the treatment of metastatic colon or rectum carcinomas that have recurred or progressed within six months following first-line therapy of 5-FU/LV and irinotecan. Eloxatin received FDA approval faster than any other cancer treatment to date. It was approved under a special FDA program enabling the promising, and much needed, drug to be sold prior to proof of its ability to prevent or delay death.
Colorectal cancer, according to the American Cancer Society, is the second leading cause of malignancy-related death in the US, and there has been very little available in the way of effective treatment for patients with advanced stages of this disease. Eloxatin may provide a worth while option where there previously was none.
Eloxatin was released in France in 1996 and Europe in 1999. It is currently marketed in over 55 countries and continues to be studied for new indications.
Powder for solution for infusion: ELOXATIN is supplied in vials containing 50 mg or 100 mg of oxaliplatin as a sterile, preservative-free lyophilized powder for reconstitution. Lactose monohydrate is present as an inactive ingredient at 450 mg and 900 mg in the 50 mg and 100 mg dosage strengths, respectively.
Concentrate for solution for infusion: ELOXATIN is supplied in vials containing 50 mg, 100 mg or 200 mg of oxaliplatin as a sterile, preservative-free, aqueous solution at a concentration of 5 mg/ml. Water for Injection, USP is present as an inactive ingredient.
ERBITUX
Erbitux is a chimeric (mouse/human) monoclonal antibody, an epidermal growth factor receptor (EGFR) inhibitor, given by intravenous infusion for treatment of metastatic colorectal cancer and head and neck cancer.
ERLOTINIB
Erlotinib hydrochloride marketed in the United States by Genentech and OSI Pharmaceuticals and elsewhere by Roche under the tradename Tarceva is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer.
Erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase, which is highly expressed and occasionally mutated in various forms of cancer. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor.
Erlotinib has shown a survival benefit in the treatment of lung cancer in phase III trials. It has been approved for the treatment of locally advanced or metastatic non-small cell lung cancer that has failed at least one prior chemotherapy regimen.
ETOPOSIDE
Etoposide is used to treat cancer of the testicles, acute monocytic and myelomonocytic leukaemia, Hodgkin's disease and certain types of lung cancer. It is also used to treat some other kinds of cancer in both males and females. Vepesid interferes with the growth of the cancer cells and eventually destroy them.
Etoposide mechanism of action results by exerting its anticancer effects by inhibiting the enzyme topoisomerase, which ultimately leads to un-repaired breaks in cellular DNA.
EULEXIN
Eulexin capsules have been approved for the treatment of locally confined Stage B2-C carcinoma of the prostate in combination with LHRH agonists and radiation therapy. Eulexin is currently marketed in the United States for the treatment of advanced (Stage D2) prostate cancer in combination with LHRH agonists.
FARESTON
Fareston is indicated for treatment of metastatic breast cancer in postmenopausal women with estrogen-receptor–positive or unknown tumors.
Fareston was approved by the U.S. Food and Drug Administration for use in October 1995.
FEMARA
Femara has been approved for the first-line treatment of postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer.
The drug is a once-a-day oral treatment originally approved in 1997 for advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.
FLUTAMIDE
Flutamide marketed by Schering-Plough under the brand name of Eulexin(also known as Flutamin) is an oral nonsteroidal antiandrogen drug primarily used to treat prostate cancer. It competes with testosterone and its powerful metabolite, dihydrotestosterone (DHT) for binding to androgen receptors in the prostate gland there by preventing them from stimulating the prostate cancer cells to grow.
Unlike the hormones with which it competes, flutamide is not a steroid rather, it is a substituted anilide. It has been largely replaced by a newer member of this class, bicalutamide, due to a better side-effect profile.
GEMCITABINE
Gemcitabine is a nucleoside analog used as chemotherapy. It is marketed as Gemzar by Eli Lilly and Company.
Pharmacology:
Chemically gemcitabine is a nucleoside analog in which the hydrogen atoms on the 2' carbons of deoxycytidine are replaced by fluorine atoms.
As with fluorouracil and other analogues of pyrimidines, the triphosphate analogue of gemcitabine replaces one of the building blocks of nucleic acids, in this case cytidine, during DNA replication. The process arrests tumor growth, as new nucleosides cannot be attached to the "faulty" nucleoside, resulting in apoptosis.
Another target of gemcitabine is the enzyme ribonucleotide reductase (RNR). The diphosphate analogue binds to RNR active site and inactivates the enzyme irreversibly. Once RNR is inhibited, the cell cannot produce the deoxyribonucleotides required for DNA replication and repair, and cell apoptosis is induced.[1]
GEMZAR
Gemzar (gemcitabine) is a nucleoside analog used as chemotherapy. It is marketed as Gemzar by Eli Lilly and Company.
Pharmacology:
Chemically gemcitabine is a nucleoside analog in which the hydrogen atoms on the 2' carbons of deoxycytidine are replaced by fluorine atoms.
As with fluorouracil and other analogues of pyrimidines, the triphosphate analogue of gemcitabine replaces one of the building blocks of nucleic acids, in this case cytidine, during DNA replication. The process arrests tumor growth, as new nucleosides cannot be attached to the "faulty" nucleoside, resulting in apoptosis.
Another target of gemcitabine is the enzyme ribonucleotide reductase (RNR). The diphosphate analogue binds to RNR active site and inactivates the enzyme irreversibly. Once RNR is inhibited, the cell cannot produce the deoxyribonucleotides required for DNA replication and repair, and cell apoptosis is induced.[1]
GLEEVEC
GLEEVEC® (imatinib mesylate) is indicated for the treatment of:
-----Newly diagnosed adult patients with Philadelphia chromosome–positive chronic myeloid leukemia(Ph+CML)in the chronic phase (CP)
-----Patients with Ph+ CML in blast crisis (BC), accelerated phase (AP), or in CP after failure of interferon-alpha therapy
-----Adult patients with relapsed or refractory Ph+ acute lymphoblastic leukemia (Ph+ ALL)
-----Adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene rearrangements
-----Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-KIT mutation or with c-KIT mutational status unknown
-----Adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase–negative or unknown
-----Adult patients with unresectable, recurrent, and/or metastatic dermatofibrosarcoma protuberans (DFSP)
-----Patients with KIT (CD117)–positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST)
-----Adjuvant treatment of adult patients following resection of KIT (CD117)–positive GIST
GLUTOXIM
NOV-002 in the USA, tradename of Glutoxim in Russia a glutathione disulfide mimetic, is currently in a pivotal Phase 3 clinical trial in advanced non-small cell lung cancer. In clinical trials conducted to date, NOV-002 administered in combination with standard chemotherapeutic regimens has resulted in increased efficacy survival, tumor response) and improved tolerance of standard chemotherapy (e.g. enhanced hematological recovery, immune stimulation). Glutoxim is manufactured in the USA by Novelos Therapeutics under the tradename of NOV-002.
GOSERELIN
Goserelin acetate available under brand name of Zoladex is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist) also known as a lutenizing hormone releasing hormone (LHRH) agonist. Goserelin acetate is used to suppress production of the sex hormones (testosterone and estrogen), particularly in the treatment of breast and prostate cancer.
Prostate cancer cells and some breast cancer cells are hormone-dependent, that is, they need hormone stimulation to grow. When the hormones are eliminated, the cancer cells are inhibited.
Zoladex approved by the U.S. Food and Drug Administration in 1989 for treatment of prostate cancer.
HERCEPTIN
Trastuzumab (INN; trade name Herceptin) is a monoclonal antibody that interferes with the HER2/neu receptor.
The HER receptors are proteins that are embedded in the cell membrane and communicate molecular signals from outside the cell to inside the cell, and turn genes on and off. The HER proteins regulate cell growth, survival, adhesion, migration, and differentiation—functions that are amplified or weakened in cancer cells. In some cancers, notably some breast cancers, HER2 is stuck in the "on" position, and causes breast cells to reproduce uncontrollably, causing breast cancer.[1]
Antibodies are molecules from the immune system that bind selectively to different proteins. Trastuzumab is an antibody that binds selectively to the HER2 protein. When it binds to defective HER2 proteins, the HER2 protein no longer causes cells in the breast to reproduce uncontrollably. This increases the survival of people with cancer. However, cancers usually develop resistance to trastuzumab.
The original studies of trastuzumab showed that it improved survival in late-stage (metastatic) breast cancer, but there is controversy over whether trastuzumab is effective in earlier stage breast cancer.[citation needed] Trastuzumab is also controversial because of its cost, as much as $100,000 per year[2], and while certain private insurance companies in the U.S. and government health care systems in Canada, the U.K. and elsewhere have refused to pay for trastuzumab for certain patients, some companies have since accepted trastuzumab treatment as a covered preventative treatment.[3]
Trastuzumab was originally developed in mice, as a mouse antibody. Because humans have immune reactions to mouse proteins, it was later developed into a human (humanized) antibody. Because the antibodies were produced from one cell that was grown into a clone of identical cells, it is called a monoclonal antibody.
Trastuzumab is also being studied for use with other cancers.[4] It has been used with some success in women with uterine papillary serous carcinomas that overexpress HER2/neu
IMATINIB
GLEEVEC® (imatinib mesylate) is indicated for the treatment of:
-----Newly diagnosed adult patients with Philadelphia chromosome–positive chronic myeloid leukemia (Ph+ CML) in the chronic phase (CP)
-----Patients with Ph+ CML in blast crisis (BC), accelerated phase (AP), or in CP after failure of interferon-alpha therapy
-----Adult patients with relapsed or refractory Ph+ acute lymphoblastic leukemia (Ph+ ALL)
-----Adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene rearrangements
-----Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-KIT mutation or with c-KIT mutational status unknown
-----Adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase–negative or unknown
-----Adult patients with unresectable, recurrent, and/or metastatic dermatofibrosarcoma protuberans (DFSP)
-----Patients with KIT (CD117)–positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST)
-----Adjuvant treatment of adult patients following resection of KIT (CD117)–positive GIST
IXEMPRA
Ixabepilone (INN; also known as azaepothilone B, codenamed BMS-247550) is an epothilone B analog[1] developed by Bristol-Myers Squibb as a cancer drug.
It is produced by Sorangium cellulosum.[2]
Contents
1 Pharmacology
2 Approval
3 Clinical uses
4 References
5 External links
Pharmacology
It acts to stabilize microtubules.[3][4]
Approval
On October 16, 2007, the U.S. Food and Drug Administration approved ixabepilone for the treatment of aggressive metastatic or locally advanced breast cancer no longer responding to currently available chemotherapies.[5] In November 2008, the EMEA has refused a marketing authorisation for Ixabepilone.[6]
Ixabepilone is administered through injection, and is marketed under the trade name Ixempra.
Clinical uses
Ixabepilone, in combination with capecitabine, has demonstrated effectiveness in the treatment of metastatic or locally advanced breast cancer in patients after failure of an anthracycline and a taxane.[7]
It has been investigated for use in treatment of non-Hodgkin's lymphoma.[8]
References:
1. Goodin S (May 2008). "Novel cytotoxic agents: epothilones". Am J Health Syst Pharm 65 (10 Suppl 3): S10–5. doi:10.2146/ajhp080089. PMID 18463327. http://www.ajhp.org/cgi/pmidlookup?view=long&pmid=18463327.
2. Lee FY, Borzilleri R, Fairchild CR, et al (December 2008). "Preclinical discovery of ixabepilone, a highly active antineoplastic agent". Cancer Chemother. Pharmacol. 63 (1): 157–66. doi:10.1007/s00280-008-0724-8. PMID 18347795.
3. Denduluri N, Swain SM (March 2008). "Ixabepilone for the treatment of solid tumors: a review of clinical data". Expert Opin Investig Drugs 17 (3): 423–35. doi:10.1517/13543784.17.3.423. PMID 18321240. http://www.expertopin.com/doi/abs/10.1517/13543784.17.3.423.
4. Goodin S (November 2008). "Ixabepilone: a novel microtubule-stabilizing agent for the treatment of metastatic breast cancer". Am J Health Syst Pharm 65 (21): 2017–26. doi:10.2146/ajhp070628. PMID 18945860. http://www.ajhp.org/cgi/pmidlookup?view=long&pmid=18945860.
5. Medical News Today
6. London, 20 November 2008 Doc. Ref. EMEA/602569/2008
7. Thomas ES, Gomez HL, Li RK, et al (November 2007). "Ixabepilone plus capecitabine for metastatic breast cancer progressing after anthracycline and taxane treatment". J. Clin. Oncol. 25 (33): 5210–
8. Aghajanian C, Burris HA, Jones S, et al (March 2007). "Phase I study of the novel epothilone analog ixabepilone (BMS-247550) in patients with advanced solid tumors and lymphomas". J. Clin. Oncol. 25 (9): 1082–8. doi:10.1200/JCO.2006.08.7304. PMID 17261851. http://www.jco.org/cgi/pmidlookup?view=long&pmid=17261851.
LETROZOLE
Letrozole available under trade name of Femara is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast cancer.
Letrozole is approved by the United States Food and Drug Administration (FDA) for the treatment of local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status in postmenopausal women.
It has been used for ovarian stimulation by fertility doctors since 2001 having less side-effects than clomiphene citrate (Clomid).
MEGACE
Megace is a man-made chemical similar to the female hormone progesterone.
Megace is used to treat loss of appetite and weight loss because of disease. It is also used in the treatment of advanced breast cancer and endometrial cancer.
MEGESTROL
Megestrol available under the trade name of Megace is a progesterone derivative with antineoplastic properties used in the treatment of advanced carcinoma of the breast and endometrium. When given in relatively high doses, Megestrol can substantially increase appetite in most individuals, even those with advanced cancer.
Megestrol Acetate Oral Suspension (a form of Megestrol) is used primarily as an appetite enhancer. The method of appetite enhancement is not known, but it can cause high blood sugar.
NEXAVAR
Nexavar is a multikinase inhibitor targeting a number of serine/threonine and receptor tyrosine kinases. Inhibition of these systems inhibits division and growth of tumor cells and potentiates cellular apoptosis.
Nexavar is specifically indicated for the treatment of advanced renal cell carcinoma (RCC).
ONDANSETRON
Ondansetron or GlaxoSmithKline's Zofran is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy.It reduces the activity of the vagus nerve, which activates the vomiting center in the medulla oblongata and also blocks serotonin receptors in the chemoreceptor trigger zone.
Early studies have also examined ondansetron as a possible treatment for psychosis resulting from advanced Parkinson's disease. It also lowers the cravings for alcohol, especially in early-onset alcoholics.
Do not use this medication if you have liver disease or allergic to ondansetron hydrochloride, to similar medicines such as dolasetron (Anzemet), granisetron (Kytril), palonosetron(Aloxi) or a personal/family history of Long QT syndrome.
OXALIPLATIN
Oxaliplatin is a coordination complex that is used in cancer chemotherapy. These platinum-based drugs are usually classified as alkylating agents, although they are actually alkylating groups (they function by a similar mechanism). Oxaliplatin was discovered in 1976 at Nagoya City University by Professor Yoshinori Kidani, who was granted U.S. Patent 4,169,846 in 1979. Oxaliplatin was subsequently in-licensed by Debiopharm and developed as an advanced colorectal cancer treatment. Debio licensed the drug to Sanofi-Aventis in 1994. Eloxatin gained European approval in 1996 (firstly in France) and approval by the U.S. Food and Drug Administration (FDA) in 2002.
The compound features a square planar platinum(II) center. In contrast to cisplatin and carboplatin, oxaliplatin features the bidentate ligand 1,2-diaminocyclohexane in place of the two monodentate ammine ligands. It also features a bidentate oxalate group.
Mechanism of action:
The cytotoxicity of platinum compounds is thought to result from inhibition of DNA synthesis in cancer cells. In vivo studies showed that Oxaliplatin has anti-tumor activity against colon carcinoma through its (non-targeted) cytotoxic effects.
PACLITAXEL
Paclitaxel sold under the trademark of Taxol is a mitotic inhibitor used in cancer chemotherapy. In this formulation, paclitaxel is dissolved in Cremophor EL and ethanol, as a delivery agent. A newer formulation, in which paclitaxel is bound to albumin, is sold under the trademark Abraxane.
Paclitaxel is now used to treat patients with lung, ovarian, breast cancer, head and neck cancer and advanced forms of Kaposi's sarcoma. It is also used for the prevention of restenosis.
Paclitaxel stabilizes microtubules and as a result interferes with the normal breakdown of microtubules during cell division. Together with docetaxel, it forms the drug category of the taxanes.
PAMIDRONATE
Pamidronate marketed by Novartis under brand name of Aredia is a nitrogen containing bisphosphonate which is used to prevent osteoporosis. It is also used to strengthen bone in Paget's disease, to prevent bone loss due to steroid use and in certain cancers with high propensity to bone, such as multiple myeloma. In multiple myeloma, it is usually administered as an intravenous infusion, lasting about 3 hours.
Due to its ability to sequester calcium in bone, it is also used to treat high calcium levels and as an experimental treatment of the bone disorder known as Osteogenesis Imperfecta or brittle bones.
REVLIMID
Lenalidomide (pronounced /lɛnəˈlɪdɵmaɪd/), initially known as CC-5013 and marketed as Revlimid by Celgene, is a derivative of thalidomide introduced in 2004. It was initially intended as a treatment for multiple myeloma, for which thalidomide is an accepted therapeutic modality, but has also shown efficacy in the class of hematological disorders known as myelodysplastic syndromes (MDS). Revlimid is also known as Revamid in the UK.
The exact mechanism of the immunomodulatory drugs (i.e., thalidomide, CC-4047/Actimid and lenalidomide) is not known. Apart from interfering with the immune system, they are also thought to act on angiogenesis.
Lenalidomide and bortezomib are considered therapeutic breakthroughs in myeloma, which generally carries a poor prognosis.
Contents [hide]
1 Mechanism of action
2 Treatment of multiple myeloma
2.1 Use in USA
2.2 Use in the UK
3 Treatment of myelodysplastic syndromes (MDS)
4 Treatment of other cancers
5 Risks
6 References
7 Further reading
8 External links
[edit] Mechanism of action
Lenalidomide has been used to successfully treat both inflammatory disorders and cancers in the past 10 years. There are multiple mechanisms of action, and they can be simplified by organizing them as mechanisms of action in vitro and in vivo.[1] In vitro, lenalidomide has three main activities: direct anti-tumour effect, inhibition of the microenvironment support for tumour cells, and immunomodulatory role. In vitro, lenalidomide induces tumour cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity. Lenalidomide has a broad range of activities that can be exploited to treat many hematologic and solid cancers.
[edit] Treatment of multiple myeloma
Multiple myeloma is a rare cancer of the blood, characterized by accumulation of a plasma cell clone in the bone marrow.[2] Lenalidomide is one of the novel drug agents used to treat multiple myeloma. It is a small molecular analogue of thalidomide that was originally found based on its ability to effectively inhibit tumour necrosis factor production. Lenalidomide is 50,000 times more potent than thalidomide in inhibiting tumour necrosis factor-alpha, and has less severe adverse drug reactions. In a phase III clinical study, Weber et al. found that lenalidomide plus dexamethasone in patients with relapsed or refractory multiple myeloma was superior to the old treatment of multiple myeloma consisting of high-dose dexamethasone alone.[3]
Nonetheless, lenalidomide, like its parent compound thalidomide, causes venous thromboembolism (VTE), a potentially serious complication with their use. Bennett et al. have reviewed incidents of lenalidomide-associated VTE among patients with multiple myeloma.[4] They have found that there are high rates of VTE when patients with multiple myeloma received thalidomide or lenalidomide in conjunction with dexamethasone, melphalan, or doxorubicin. When lenalidomide and dexamethasone are used to treat multiple myeloma, a median of 14% of patients had VTE (range,3-75%). Patients who took prophylaxis to treat lenalidomide-associated VTE, such as aspirin, thromboembolism rates were found to be lower than without prophylaxis, frequently lower than 10%. Clearly, thromboembolism is a serious adverse drug reaction associated with lenalidomide, as well as thalidomide. In fact, a black box warning is included in the package insert for lenalidomide, indicating that lenalidomide-dexamethasone treatment for multiple myeloma is complicated by high rates of thromboembolism.
Currently, clinical trials are underway to further test the efficacy of lenalidomide to treat multiple myeloma and how to prevent the lenalidomide associated venous thromboembolism.
[edit] Use in USA
On June 29, 2006, lenalidomide received U.S. Food and Drug Administration (FDA) clearance for use in combination with dexamethasone in patients with multiple myeloma who have received at least one prior therapy.
[edit] Use in the UK
On 23 April 2009, The National Institute for Health and Clinical Excellence (NICE) issued a Final Appraisal Determination (FAD) approving lenalidomide, in combination with dexamethasone, as an option to treat patients who suffer from multiple myeloma who have received two or more prior therapies in England and Wales. [5] [6]
[edit] Treatment of myelodysplastic syndromes (MDS)
With myelodysplastic syndromes, the best results of lenalidomide were obtained in patients with deletion 5q (List et al. 2005).
It was approved by the FDA on December 27, 2005 for patients with low or intermediate-1 risk MDS with 5q- with or without additional cytogenetic abnormalities. A completed Phase II, multi-centre, single-arm, open-label study evaluated the efficacy and safety of Revlimid monotherapy treatment for achieving haematopoietic improvement in red blood cell (RBC) transfusion dependent subjects with low- or intermediate-1-risk MDS associated with a deletion 5q cytogenetic abnormality.
63.8% of subjects had achieved RBC-transfusion independence accompanied by a median increase of 5.8 g/dL in blood Hgb concentration from baseline to the maximum value during the response period. Major cytogenetic responses were observed in 44.2% and minor cytogenetic responses were observed in 24.2% of the evaluable subjects. Improvements in bone marrow morphology were also observed. The results of this study demonstrate the efficacy of Revlimid for the treatment of subjects with Low- or Intermediate-1-risk MDS and an associated del 5 cytogenetic abnormality.[7][8][9]
This section requires expansion.
[edit] Treatment of other cancers
Lenalidomide is undergoing clinical trial as a treatment for Hodgkin's Lymphoma[10], as well as non-Hodgkin's Lymphoma, Chronic Lymphocytic Leukemia and solid tumor cancers, such as carcinoma of the pancreas. [11]
[edit] Risks
Lenalidomide is related to thalidomide which is known to be teratogenic. While laboratory tests have suggested lenalidomide is not teratogenic it is categorized as such because of its structural similarities with thalidomide. It therefore has the pregnancy category X and cannot be prescribed for women who are pregnant or who might be conceiving. For this reason, the drug is only available through a restricted distribution system called RevAssistSM.
Other potential side effects are thrombosis, pulmonary embolus, and hepatotoxicity, as well as bone marrow toxicity resulting in neutropenia and thrombocytopenia. Myelosuppression is the major dose-limiting toxicity, which is contrary to experience with thalidomide.[12]
In March 2008, the U.S. Food and Drug Administration (FDA) included lenalidomide on a list of 20 prescription drugs under investigation for potential safety problems. The drug is being investigated for possibly increasing the risk of developing Stevens-Johnson syndrome, a life-threatening condition affecting the skin.[13]
SORAFENIB
Sorafenib is a cancer (chemotherapeutic) medication. Sorafenib interferes with the growth of cancer cells and slows their growth and spread in the body.
Sorafenib is used to treat a type of kidney cancer called advanced renal cell carcinoma. It is also used to treat liver cancer.
SPRYCEL
Dasatinib, also known as BMS-354825, is a cancer drug produced by Bristol-Myers Squibb and sold under the trade name Sprycel. Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinases inhibitor approved for use in patients with chronic myelogenous leukemia (CML) after imatinib treatment and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). It is also being assessed for use in metastatic melanoma.
The drug is named after one of the inventor chemists, Jagabandhu Das, who was a member of the large discovery and development team at Bristol Myers Squibb.[1]
Contents [hide]
1 Efficacy
2 Molecular Targets
3 Duration of benefit
4 Susceptible genotypes
5 Toxicities
6 References
7 External links
[edit] Efficacy
In a Phase I dose escalation study published in June 2006, dasatinib was tested in patients who were resistant to or who could not tolerate imatinib.[2] Complete hematological responses[3] were seen in 37 of 40 patients with chronic-phase CML. Major hematologic responses[4] were seen in 31 of 44 patients with accelerated-phase CML, CML in blast crisis, or Ph+ ALL.
[edit] Molecular Targets
The main targets of dasatinib, are BCRABL, SRC, Ephrins, GFR.
[edit] Duration of benefit
Responses were maintained in 95% of patients with chronic-phase CML, with a median follow-up time of >12 months. In patients with accelerated-phase CML, 82% remained in remission, although with a median follow-up of only 5 months. Nearly all patients with CML in blast crisis or Ph+ ALL relapsed within 6 months.
[edit] Susceptible genotypes
Responses were seen in patients with all BCR/ABL genotypes, with the exception of T315I mutation, which confers resistance to both dasatinib, nilotinib and imatinib in vitro.
[edit] Toxicities
Neutropenia and myelosuppression were common toxic effects. Fifteen patients in the above-mentioned study developed pleural effusions, which were felt to be a side effect of dasatinib. Some of these patients required thoracentesis or pleurodesis to treat the effusions. Other adverse events included mild to moderate diarrhea, peripheral edema, and headache. A small number of patients developed abnormal liver function tests which returned to normal without dose adjustments. Mild hypocalcemia was also noted, but did not appear to cause any significant problems.
SUNITINIB
Sunitinib marketed as Sutent, and previously known as SU11248 is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006.
Sunitinib also inhibits KIT (CD117), the RTK that (when improperly activated by mutation) drives the majority of gastrointestinal stromal cell tumors.
Sunitinib was the first cancer drug simultaneously approved for two different indications. Sunitinib has become a standard of care for both of these cancers, and is currently being studied for the treatment of many others.
SUTENT
SUTENT is a medicine that treats 2 kinds of cancer.
1. GIST (gastrointestinal stromal tumor). This is a rare cancer of the stomach, bowel, or esophagus. SUTENT is used when the medicine
Gleevec® (imatinib mesylate) did not stop the cancer from growing OR
when you cannot take Gleevec®.
2. Advanced kidney cancer (advanced renal cell carcinoma or RCC). SUTENT may slow or stop the growth of cancer. It may help shrink tumors. SUTENT has not been studied in children.
TAMOXIFEN
Tamoxifen blocks the actions of estrogen, a female hormone. It works by blocking the effect of estrogen on certain tumors. This may prevent the growth of tumors that are activated by estrogen.
Tamoxifen is used to treat and prevent some types of breast cancer. It is used in women who are at high risk for breast cancer and in women with DCIS (after surgery and radiation).
TARCEVA
Tarceva is a Human Epidermal Growth Factor Receptor Type 1/Epidermal Growth Factor Receptor (HER1/EGFR) tyrosine kinase inhibitor.
Tarceva appears to impede cell-cell singlaling pathways which have been implicated in rapid cell division and survival. Overactivation of these pathways are thought to be central to tumor growth and metastasis.
It is specifically indicated as monotherapy to treat non-small cell lung cancer in patients who have failed to respond or has ceased responding to at least one round of chemotherapy.
TASIGNA
Nilotinib, in the form of the hydrochloride monohydrate salt, is a tyrosine kinase inhibitor. It inhibits BCR-ABL.[1]
It was approved as Tasigna in the USA and the EU for drug-resistant chronic myelogenous leukemia (CML)[2]. In June 2006, a Phase I clinical trial found nilotinib, also known by its clinical code AMN107, has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib (Gleevec), another tyrosine kinase inhibitor currently used as a first-line treatment.[3] In that study 92% of patients (already resistant or unresponsive to Gleevec) achieved a normal white blood cell counts after five months of treatment.[4] The drug carries a black box warning for possible heart complications.[5][6]
References:
^ Weisberg E, Manley P, Mestan J, Cowan-Jacob S, Ray A, Griffin JD (June 2006). "AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL". Br. J. Cancer 94 (12): 1765–9. doi:10.1038/sj.bjc.6603170. PMID 16721371.
^ Novartis 29/10/2007 Press Release.
^ Kantarjian H et al. (2006). "Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL". N Engl J Med 354 (24): 2542–51. doi:10.1056/NEJMoa055104. PMID 16775235.
^ "Patients with treatment-resistant leukemia achieve high responses to Tasigna (nilotinib) in first published clinical trial results". MediaReleases (Novartis). 2006-06-14. http://cws.huginonline.com/N/134323/PR/200606/1056533_5.html. Retrieved 2009-08-04.
^ "FDA Approves Tasigna for Treatment of Philadelphia Chromosome Positive Chronic Myeloid Leukemia". U.S. Food and Drug Administration. 2007-10-30. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/2007/ucm109017.htm. Retrieved 2009-08-04.
^ "Prescribing information for Tasigna (nilotinib) Capsules" (PDF). NDA 022068. U.S. FDA. 2007-10-29. http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022068lbl.pdf. Retrieved 2009-08-04.
TAXOL
The U.S. Food and Drug Administration approved Bristol-Myers Squibb's cancer drug Taxol for the treatment of AIDS-related Kaposi's Sarcoma.
Taxol therapy reduces the size of patients tumors and diminishes their symptoms and pain. Taxol helped a majority of patients who had failed other therapies.
TAXOTERE
Taxotere has been approved as a treatment for subjects who have locally advanced or metastatic (spreading) breast cancer, which has progressed during anthracycline-based therapy or has relapsed during anthracycline-based adjuvant therapy.
Approximately two out of three breast cancer subjects treated with chemotherapy in the United States receive anthracyclines at some point in the treatment of their disease.
TEMODAR
Temodar capsules have been approved for the treatment of adult patients with refractory anaplastic astrocytoma. Temodar is the first new chemotherapy agent for this type of brain tumor approved in the U.S. in 20 years.
The median survival time for patients with this disease ranges from two to three years from the time of initial diagnosis.
TEMOZOLOMIDE
Temozolomide available under brand name of Temodar is an oral alkylating agent which can be used for the treatment of Grade IV astrocytoma which is an aggressive brain tumor also known as glioblastoma multiforme.
Temozolomide is an imidazotetrazine derivative of the alkylating agent dacarbazine. It undergoes rapid chemical conversion in the systemic circulation at physiological pH to the active compound, MTIC (monomethyl triazeno imidazole carboxamide). Temozolomide exhibits schedule-dependent antineoplastic activity by interfering with DNA replication.
It has been available in the US since August 1999, and in other countries since the early 2000s.
TOREMIFENE
Toremifene citrate available under brand name of Acapodene is an oral selective estrogen receptor modulator (SERM) which helps oppose the actions of estrogen in the body. Licensed in the United States under the brand name Fareston, toremifene citrate is FDA approved for use in advanced (metastatic) breast cancer.
GTx Inc. is currently conducting two different phase 3 clinical trials. First, a pivotal Phase clinical trial for the treatment of serious side effects of androgen deprivation therapy (especially vertebral/spine fractures and hot flashes, lipid profile, and gynecomastia) for advanced prostate cancer and second, a pivotal Phase III clinical trial for the prevention of prostate cancer in high risk men with high grade prostatic intraepithelial neoplasia.
TRASTUZUMAB
Trastuzumab (INN; trade name Herceptin) is a monoclonal antibody that interferes with the HER2/neu receptor.
The HER receptors are proteins that are embedded in the cell membrane and communicate molecular signals from outside the cell to inside the cell, and turn genes on and off. The HER proteins regulate cell growth, survival, adhesion, migration, and differentiation—functions that are amplified or weakened in cancer cells. In some cancers, notably some breast cancers, HER2 is stuck in the "on" position, and causes breast cells to reproduce uncontrollably, causing breast cancer.[1]
Antibodies are molecules from the immune system that bind selectively to different proteins. Trastuzumab is an antibody that binds selectively to the HER2 protein. When it binds to defective HER2 proteins, the HER2 protein no longer causes cells in the breast to reproduce uncontrollably. This increases the survival of people with cancer. However, cancers usually develop resistance to trastuzumab.
The original studies of trastuzumab showed that it improved survival in late-stage (metastatic) breast cancer, but there is controversy over whether trastuzumab is effective in earlier stage breast cancer.[citation needed] Trastuzumab is also controversial because of its cost, as much as $100,000 per year[2], and while certain private insurance companies in the U.S. and government health care systems in Canada, the U.K. and elsewhere have refused to pay for trastuzumab for certain patients, some companies have since accepted trastuzumab treatment as a covered preventative treatment.[3]
Trastuzumab was originally developed in mice, as a mouse antibody. Because humans have immune reactions to mouse proteins, it was later developed into a human (humanized) antibody. Because the antibodies were produced from one cell that was grown into a clone of identical cells, it is called a monoclonal antibody.
Trastuzumab is also being studied for use with other cancers.[4] It has been used with some success in women with uterine papillary serous carcinomas that overexpress HER2/neu.[5]
TYKERB
Lapatinib (INN), used in the form of lapatinib ditosylate, (USAN) (Tykerb/Tyverb, GSK) is an orally active drug for breast cancer and other solid tumours.[1] It is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.[2] It is used in combination therapy for HER2-positive breast cancer. It has been approved as front-line therapy in triple positive breast cancer and as an adjuvant therapy when patients have progressed on Herceptin.[3]
VELCADE
Velcade is an antineoplastic agent available for intravenous injection. The proteasome is an enzyme complex that exists in all cells and plays an important role in degrading proteins that control the cell cycle and cellular processes. By blocking the proteasome, Velcade disrupts numerous biologic pathways, including those related to the growth and survival of cancer cells.
Velcade for Injection is indicated for the treatment of multiple myeloma patients who have received at least two prior therapies and have demonstrated disease progression on the last therapy.
VEPESID
Vepesid belongs to the group of medicines known as antineoplastic agents. It is used to treat cancer of the testicles and certain types of lung cancer.
It is also sometimes used to treat some other kinds of cancer in both males and females.
VIDAZA
Azacitidine (INN) or 5-azacytidine, sold under the trade name Vidaza, is a chemical analogue of cytidine, a nucleoside present in DNA and RNA. Azacitidine and its deoxy derivative, decitabine (also known as 5-aza-2¡ädeoxycytidine), are used in the treatment of myelodysplastic syndrome. Both drugs were first synthesized in Czechoslovakia as potential chemotherapeutic agents for cancer.
Contents [hide]
1 Uses
2 Mechanism of action
3 See also
4 References
5 External links
Uses
Azacitidine is mainly used in the treatment of myelodysplastic syndrome (MDS), for which it received approval by the U.S. Food and Drug Administration on May 19, 2004; it is marketed as Vidaza. In a randomized controlled trial comparing azacitidine to supportive treatment of MDS, around 16% of people receiving the drug had a complete or partial response¡ªblood cell counts and bone marrow morphology returning to normal¡ªand 2/3 patients who required blood transfusions before the study no longer needed them after receiving azacitidine.
It can also be used in vitro to remove methyl groups from DNA. This may weaken the effects of gene silencing mechanisms that occurred prior to the methylation. Methylation events are therefore believed to secure the DNA in a silenced state. Demethylation may reduce the stability of silencing signals and thus confer relative gene activation.
Mechanism of action:
Cells in the presence of azacitidine incorporate it into DNA during replication and RNA during transcription. The incorporation of azacitidine into DNA or RNA inhibits methyltransferase thereby causing demethylation in that sequence, affecting the way that cell regulation proteins are able to bind to the DNA/RNA substrate. Inhibition of DNA methylation occurs through the formation of stable complexes between the molecule and with DNA methyltransferases, thereby saturating the cells methylation machinery.
XELODA
Xeloda has been approved for use as a first-line treatment for subjects with metastatic colorectal cancer when treatment with fluoropyrimidine therapy alone is preferred.
Xeloda is available in tablet formulation, which provides significantly more convenience in dosing compared to other more complex intravenous chemotherapy regimens.
ZOFRAN
An intramuscular administration of Zofran for postoperative nausea and vomiting in adults has been approved by the FDA.
Normally, Zofran is given through an IV injection or in tablet form. This new intramuscular (IM) administration bypasses difficulties some patients may encounter.
ZOLADEX
Zoladex is a hormone similar to the one normally released from the hypothalamus gland in the brain. It is used to treat Cancer of the prostate in men, breast cancer in women if it develops before or around the time of menopause, endometriosis, thinning of the lining of the uterus before surgery on the uterus.
ZOLEDRONIC ACID
Zoledronic acid injection is a treatment for hypercalcemia of malignancy (HCM; a condition resulting in high calcium blood levels due to cancer). Zolendronic acid is also used to reduce and delay bone complications due to multiple myeloma and bone metastases from solid tumors; used with anti-cancer medicines. Zolendronic acid is not an anti-cancer therapy. If you have prostate cancer, you should have failed treatment with at least one hormonal therapy prior to taking Zolendronic acid.
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