Lorbrena Tablets
Lorlatinib
25 mg
PFIZER CANADA INC.
| Pack size | 30's HDPE Bottle |
|---|---|
| Dispensing mode | POM |
| Source | CANADA |
| Agent | Modern Pharmaceutical Co. |
| Retail Price | 14506.50 AED |
Available as:
Indications
Lorbrena Tablets is used for:
Non-small Cell Lung Cancer
Adult Dose
Non-small Cell Lung Cancer
Indications
Indicated for patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) whose disease has progressed on the following
Crizotinib and at least 1 other ALK inhibitor, OR
Alectinib or ceritinib as first ALK inhibitor therapy
100 mg PO qDay with or without food
Continue until disease progression or unacceptable toxicity
Hepatic impairment
Mild (total bilirubin ?ULN with AST >ULN or total bilirubin >1-1.5x ULN with any AST): No dose adjustment necessary
Moderate or severe: Recommended dose not established
Child Dose
Renal Dose
Renal impairment
Mild or moderate (CrCl 30-89 mL/min): No dosage adjustment necessary
Severe (CrCl <30 mL/min): Recommended dose not established
Administration
Contra Indications
Coadministration with strong CYP3A inducers
Precautions
Severe hepatotoxicity occurred in healthy subjects receiving lorlatinib with rifampin, a strong CYP3A inducer; consider discontinuing lorlatinib or CYP3A inducer for persistent Grade ≥2 hepatotoxicity (see Contraindications)
CNS effects (eg, seizures, hallucinations, changes in cognitive function, mood [including suicidal ideation]) may occur Increased serum cholesterol and triglycerides may occur; initiate or increase dose of lipid-lowering agents in patients with hyperlipidemia; monitor serum cholesterol and triglycerides
PR interval prolongation and AV block reported; monitor ECG before initiating treatment and periodically thereafter
Severe or life-threatening pulmonary adverse reactions consistent with ILD/pneumonitis can occur
Pregnancy-Lactation
Pregnancy
Based on findings from animal studies and its mechanism of action, embryo-fetal harm may occur when administered to a pregnant woman
No available data on use in pregnant women
Advise pregnant women of the potential risk to fetus
Verify pregnancy status in females of reproductive potential before initiating treatment
Animal data
Administration of lorlatinib to pregnant rats and rabbits by oral gavage during organogenesis resulted in malformations, increased postimplantation loss, and abortion at maternal exposures that were equal to or less than the human exposure at 100 mg qDay
Contraception
Female patients of reproductive potential: Use effective nonhormonal contraception during treatment and for at least 6 months after final dose, because lorlatinib can render hormonal contraceptives ineffective
Males: Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective contraception during treatment and for at least 3 months after final dose
Infertility
Based on animal studies, male fertility may transiently be impaired
Lactation
No data on presence of lorlatinib or its metabolites in either human or animal milk or its effects on the breastfed infant or on milk production
Because of potential for serious adverse reactions in breastfed infants, instruct women not to breastfeed during treatment and for 7 days after final dose
Interactions
CYP3A4 inducers
Coadministration with strong CYP3A inducers decrease lorlatinib plasma concentrations
Effect of moderate CYP3A inducer on lorlatinib plasma concentrations not studied; if coadministration unavoidable, monitor ALT, AST, and bilirubin
CYP3A4 inhibitors
Coadministration with strong CYP3A inhibitors increased lorlatinib plasma concentrations
CYP3A substrates
Coadministration with CYP3A substrates decreases concentration of CYP3A substrates, which may reduce the efficacy of these substrates
Avoid use with CYP3A substrates with narrow therapeutic index; if coadministration unavoidable, increase dose of CYP3A substrate in accordance to prescribing information
Adverse Effects
Side effects of Lorlatinib :
>10%
Hypercholesterolemia (96%)
Hypertriglyceridemia (90%)
Edema (57%)
Hyperglycemia (52%)
Anemia (52%)
Peripheral neuropathy (47%)
Increased AST (37%)
Hypoalbuminemia (33%)
Increased ALT (28%)
Cognitive effects (27%)
Dyspnea (27%)
Fatigue (26%)
Weight gain (24%)
Increased lipase (24%)
Increased alkaline phosphatase (24%)
Thrombocytopenia (23%)
Arthralgia (23%)
Mood effects (23%)
Diarrhea (22%)
Increased amylase (22%)
Lymphopenia (22%)
Hyperkalemia (21%)
Hypomagnesemia (21%)
Headache (18%)
Cough (18%)
Nausea (18%)
Myalgia (17%)
Dizziness (16%)
Vision disorder (15%)
Constipation (15%)
Rash (14%)
Back pain (13%)
Pain in extremity (13%)
Vomiting (12%)
Speech effects (12%)
Pyrexia (12%)
Upper respiratory tract infection (12%)
Grades 3 or 4
Hypercholesterolemia (18%)
Hypertriglyceridemia (18%)
Mechanism of Action
ALK/ROS1 tyrosine kinase inhibitor
ALK and ROS1 kinases promote tumor progression in ALK/ROS1 positive lung cancer; lorlatinib binds to and inhibits both kinases, which leads to a disruption of the ALK- and ROS1-mediated signaling; this disruption can subsequently inhibit tumor cell growth in ALK- and ROS1-overexpressing tumor cells
Note
Lorbrena 25 mg Tablets manufactured by PFIZER CANADA INC.. Its generic name is Lorlatinib. Lorbrena is availble in United Arab Emirates.
Farmaco UAE drug index information on Lorbrena Tablets is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.