Alecensa Capsules
Alectinib
150mg
F. Hoffmann-La Roche Ltd.
| Pack size | 224 (4 Packs x 56's) Capsules |
|---|---|
| Dispensing mode | POM |
| Source | SWITZERLAND |
| Agent | CITY MEDICAL STORE |
| Retail Price | 31213.00 AED |
Indications
Alecensa Capsules is used for:
Non-small Cell Lung Cancer, Indicated for anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer (NSCLC)
ALK-positive, locally advanced or metastatic NSCLC who have progressed on or are intolerant to crizotinib.
Adult Dose
Non-small Cell Lung Cancer
600 mg PO BID until disease progression or unacceptable toxicity
Dose reduction schedule
Starting dose: 600 mg PO BID
First dose reduction: 450 mg PO BID
Second dose reduction: 300 mg PO BID
Discontinue if patients are unable to tolerate 300 mg PO BID
Nephrotoxicity
Grade 3: Temporarily withhold until serum creatinine recovers to ?1.5x ULN, then resume at reduced dose
Grade 4: Permanently discontinue
Hepatotoxicity
ALT or AST elevation >5x ULN with total bilirubin (TB) ?2x ULN: Temporarily withhold until recovery to baseline or to ?3 times ULN, then resume at reduced dose
ALT or AST elevation >3x ULN with TB elevation >2x ULN in absence of cholestasis or hemolysis: Permanently discontinue
TB elevation >3x ULN: Temporarily withhold until recovery to baseline or to ?1.5x ULN, then resume at reduced dose
Hepatic impairment
Mild (TB ?ULN and AST >ULN or TB >1-1.5x ULN and any AST): No dose adjustment required
Moderate-to-severe: Not studied
Child Dose
Renal Dose
Renal impairment
Mild-to-moderate: No dose adjustment required
Severe (CrCl <30 mL/min) or ESRD: Not studied
Administration
Should be taken with food: Swallow whole, do not open/dissolve the cap.
Contra Indications
Hypersensitivity.
Precautions
Elevated liver enzymes reported; monitor liver function tests, including ALT, AST, and total bilirubin, q2weeks during the first 2 months of treatment, then periodically during treatment, with more frequent testing in patients who develop transaminase and bilirubin elevations
Interstitial lung disease (ILD) and pneumonitis reported; promptly investigate any patient who presents with worsening respiratory symptoms (eg, dyspnea, cough, fever) and immediately withhold treatment in patients diagnosed with ILD/pneumonitis
Symptomatic bradycardia may occur; monitor heart rate and blood pressure regularly
Severe myalgia and elevated CPK reported; advise patients to report any unexplained muscle pain, tenderness, or weakness; assess CPK levels q2weeks for the first month of treatment and as clinically indicated in patients reporting symptoms
Based on findings from animal studies and its mechanism of action, alectinib can cause fetal harm when administered to pregnant women
Renal impairment occurred; incidence of Grade ≥3 renal impairment was 1.7%, of which 0.5% were fatal events
Lactation
Unknown if distributed in human breast milk
Because of the potential for serious adverse reactions in breastfed infants from alectinib, advise a lactating woman not to breastfeed during treatment and for 1 week after the final dose
Pregnancy-Lactation
Pregnancy
Based on animal studies and its mechanism of action, can cause fetal harm when administered to a pregnant woman There are no available data on use in humans during pregnancy
Animal data
Administration to pregnant rats and rabbits by oral gavage during the period of organogenesis resulted in embryo-fetal toxicity and abortion at maternally toxic doses with exposures approximately 2.7-times those observed in humans treated with alectinib at 600 mg BID
Contraception
Females: Use effective contraception during treatment and for 1 week after the final dose
Males: Use effective contraception during treatment and for 3 months following the final dose
Lactation
Unknown if distributed in human breast milk
Because of the potential for serious adverse reactions in breastfed infants from alectinib, advise a lactating woman not to breastfeed during treatment and for 1 week after the final dose
Interactions
May increase plasma conc of co-administered substrates of P-glycoprotein (P-gp) or breast cancer resistance protein (BCRP) transporters (eg, digoxin, dabigatran, methotrexate).
Adverse Effects
Side effects of Alectinib :
>10% (All Grades)
Anemia (56%)
Increased AST (51%)
Increased alkaline phosphatase (47%)
Increased CPK (43%)
Fatigue (26-41%)
Hyperbilirubinemia (39%)
Hyperglycemia (36%)
Increased ALT (34%)
Constipation (34%)
Hypocalcemia (32%)
Edema (22-30%)
Hypokalemia (29%)
Myalgia (23-29%)
Increased creatinine (28%)
Lymphopenia (22%)
Hypophosphatemia (21%)
Hyponatremia (20%)
Cough (19%)
Rash (15-18%)
Nausea (14-18%)
Headache (17%)
Diarrhea (12-16%)
Dyspnea (16%)
Back pain (12%)
Vomiting (7-12%)
Bradycardia (11%)
Increased weight (11%)
1-10% (All Grades
Vision disorder (10%)
1-10% (Grade 3 or 4)
Increased ALT (4.8%)
Increased CPK (4.6%)
Lymphopenia (4.6%)
Vision disorders (4.6%)
Hypokalemia (4%)
Renal impairment (3.9%)
Dyspnea (3.6%)
Increased AST (3.6%)
Dysgeusia (3.3%)
Hypophosphatemia (2.8%)
Hyperbilirubinemia (2.4%)
Hyperglycemia (2%)
Hyponatremia (2%)
Anemia (2%)
Fatigue (1.2%)
Myalgia (1.2%)
Diarrhea (1.2%)
Increased alkaline phosphatase (1.2%)
<1% (Grade 3 or 4)
Edema (0.7-0.8%)
Headache (0.8%)
Rash (0.4-0.7%)
Dysgeusia (0.7%)
Nausea (0.7%)
Vomiting (0.4%)
Increased weight (0.4%)
Hypocalcemia (0.4%)
Mechanism of Action
Tyrosine kinase inhibitor that targets ALK and RET
In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations
The major active metabolite of alectinib, M4, showed similar in vitro potency and activity
Alectinib and M4 demonstrated in vitro and in vivo activity against multiple mutant forms of the ALK enzyme, including some mutations identified in NSCLC tumors in patients who have progressed on crizotinib
Note
Alecensa 150mg Capsules manufactured by F. Hoffmann-La Roche Ltd.. Its generic name is Alectinib. Alecensa is availble in United Arab Emirates.
Farmaco UAE drug index information on Alecensa Capsules is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.