Alectinib - 150mg


Description


Alectinib 150mg belongs to second generation oral drug which selectively prohibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.
It is part used in the treatment of non-small cell lung cancer (NSCLC) expressing the ALK-EML4 (echinoderm microtubule-associated protein-like 4) fusion protein that causes proliferation of NSCLC cells.
Alectinib is a prescription drug which is used under guidance of medical practioners


Indication


Alectinib 150mg is used for the therapy of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC).


Dosage and administration


Non- Small Cell Lung Cancer :
The usual dose of Alectinib is 600mg PO BID until disease progression or unacceptable
Renal impairment patients dose of Alectinib is 450mg orally twice daily
Alectinib is administrated with food







Mechanism Of Action


Alectinib is a group of drugs belongs to tyrosine kinase inhibitor which targets ALK and RET.
In nonclinical studies, Alectinib prevents ALK phosphorylation and ALK-mediated energizing of the downstream signalling proteins STAT3 and AKT, andlower the tumor cell activity in multiple cell lines harbouring ALK fusions, amplifications, or activating mutations.

ADME


Absorption:
Peak plasma concentration 4 hours and bioavailability of Alectinib 37%
Distribution:
Alectinib bound to human plasma proteins 99%
Metabolism:
Metabolized by CYP3A4 to its major active metabolite M4, the main circulating moieties in plasma, total radioactivity 76% constituting.
Elimination:
In oral administration, radioactivity 98% was excreted in feces. 84% dose was excreted in the feces unchanged Alectinib.
Half-life is 33 hours

Precautions


• Due to Alectinib administration, Symptomatic bradycardia may have observed; control heart rate and blood pressure regularly
• Alectinib may causes Severe myalgia and elevated CPK resulted; advise patients to report any unexplained muscle pain, tenderness, or weakness;
• Embryo-fetal toxicity: Based on data from animal studies and its mechanism of action, Alectinib can cause fetal harm when administered to pregnant women.
• Renal impairment occurred during Alectinib treatment; incidence of Grade ≥3 renal impairment was 1.7%, of which 0.5% were fatal events.

Drug Interaction


No pharmacokinetic interactions with Alectinib 150mg needed dosage adjustment have been observed.

Side Effects


Alectinib causes some side effects while administrating certain condition as follows :
COMMON SIDE EFFECTS:
• Muscle pain
• Bradycardia
• Tiredness
• Constipation
• Anemia
• Nausea or vomiting
• Abdominal Pain on the right side
• Bleeding or bruising more easily than normal
• Hepatotoxicity
• Lung Problems
• Trouble breathing
• Shortness of breath .

Pregnancy


Based on studies of animal and mechanism of action, Alectinib 150mg will cause fetal harm when given to pregnant women
Advice the female not to become pregnant while on treatment with Alectinib

Missed Dose


If the patient vomits after taking a dose of Alectinib or missed to take a dose, then should not to take an extra dose, but to take the next dose at the regular time, skip the missed dose.



Lactation


During treatment with Alectinib, advise the women not to breastfed to infants


Storage


Store at below 300C
Store the drug in original container


Contraindication


None


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