Trepmac Tablet
Brigatinib
90 mg
Genvio Pharma Ltd.
| Pack size | 30's pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 1400.00 AED |
Indications
Trepmac Tablet is used for:
Non-Small Cell Lung Cancer
Adult Dose
Non-Small Cell Lung Cancer
Indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.
90 mg orally once daily for the first 7 days; then increase to 180 mg orally once daily.
Continue until disease progression or unacceptable toxicity
Child Dose
Renal Dose
Renal impairment
Mild or moderate (CrCl 30-89 mL/min): No dose adjustment required
Severe (CrCl 15-29 mL/min): Reduce brigatinib dose by ~50% (eg, from 180 mg to 90 mg, or from 90 mg to 60 mg)
Administration
Take with or without food
Contra Indications
Precautions
Interstitial Lung Disease (ILD)/Pneumonitis: Withhold Brigatinib for new or worsening respiratory symptoms and promptly evaluate for ILD/pneumonitis. Upon recovery, either dose reduce or permanently discontinue Brigatinib.
Hypertension: Monitor blood pressure after 2 weeks and then at least monthly during treatment. For severe hypertension, withhold Brigatinib, then dose reduce or permanently discontinue.
Bradycardia: Monitor heart rate and blood pressure regularly during treatment. If symptomatic, withhold Brigatinib, then dose reduce or permanently discontinue.
Visual Disturbance: Advise patients to report visual symptoms.
Withhold Brigatinib and obtain ophthalmologic evaluation, then dose reduce or permanently discontinue Brigatinib.
Creatine Phosphokinase (CPK) Elevation: Monitor CPK levels regularly during treatment. Based on the severity and with muscle pain or weakness, withhold Brigatinib, then resume or reduce dose.
Pancreatic Enzymes Elevation: Monitor lipase and amylase levels regularly during treatment. Based on the severity, withhold Brigatinib, then resume or reduce dose.
Hyperglycemia: Assess fasting serum glucose prior to starting Brigatinib and regularly during treatment. If not adequately controlled with optimal medical management, withhold Brigatinib, then consider dose reduction or permanently discontinue, based on severity.
Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use a non-hormonal method of effective contraception
MONITORING PARAMETERS
Monitor for new or worsening respiratory symptoms, particularly in the first week of treatment—promptly investigate if pneumonitis is suspected.
Monitor blood pressure, heart rate, creatine phosphokinase, amylase, and lipase regularly.
Monitor liver function at baseline, then every 2 weeks during the first 3 months of treatment, and periodically thereafter.
Monitor fasting serum glucose at baseline and periodically thereafter.
Pregnancy-Lactation
Pregnancy
Based on its mechanism of action and findings in animals, can cause fetal harm when administered to pregnant women
Administration to pregnant rats during the period of organogenesis resulted in dose-related skeletal anomalies at doses as low as 12.5 mg/kg/day (~0.7 times the human exposure by AUC at 180 mg once daily), as well as increased postimplantation loss, malformations, and decreased fetal body weight at doses of 25 mg/kg/day (~1.26 times the human exposure at 180 mg once daily) or greater
Infertility: Based on findings in male reproductive organs in animals, may cause reduced fertility in males
Contraception
Females: Advise females of reproductive potential to use effective nonhormonal contraception during treatment and for at least 4 months after the final dose
Counsel patients to use a nonhormonal method of contraception since brigatinib can render some hormonal contraceptives ineffective
Males: Because of the potential for genotoxicity, advise males with female partners of reproductive potential to use effective contraception during treatment and for at least 3 months after the final dose
Lactation
Unknown if distributed in human breast milk
Because of the potential for adverse reactions in breastfed infants, advise lactating women not to breastfeed during treatment and for 1 week following the final dose
Interactions
Increased plasma conc & adverse reactions w/ strong CYP3A inhibitors [eg, certain antivirals (boceprevir, cobicistat, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir), macrolide antibiotics (clarithromycin), antifungals (itraconazole, ketoconazole, posaconazole, voriconazole), conivaptan]; grapefruit or grapefruit juice.
Decreased plasma conc & efficacy w/ strong CYP3A inducers (eg, rifampin, carbamazepine, phenytoin, St. John's Wort).
Decreased conc & loss of efficacy of CYP3A substrates (eg, hormonal contraceptives).
Contraindicated (2)
doravirine
lonafarnib
Adverse Effects
Side effects of Brigatinib :
>10%
Increased AST (38%)
Hyperglycemia (38%)
Increased ALT (34%)
Nausea (33%)
Fatigue (29%)
Headache (28%)
Increased CPK (27%)
Increased amylase (27%)
Dyspnea (27%)
Vomiting (24%)
Anemia (23%)
Decreased appetite (22%)
Prolonged aPTT (22%)
Increased lipase (21%)
Diarrhea (19%)
Constipation (19%)
Lymphopenia (19%)
Cough (18%)
Abdominal pain (17%)
Increased alkaline phosphatase (15%)
Decreased phosphorous (15%)
Rash (15%)
Pyrexia (14%)
Arthralgia (14%)
Peripheral neuropathy (13%)
Muscle spasms (12%)
Hypertension (11%)
Pain in extremity (11%)
Insomnia (11%)
1-10%
Back pain (10%)
Myalgia (9.2%)
Visual disturbances (7.3%)
Pneumonia (4.6%)
Interstitial lung disease/pneumonitis (3.7%)
<1%
Hypoxia (0.9%)
Mechanism of Action
Tyrosine kinase inhibitor with in vitro activity at clinically achievable concentrations against multiple kinases, including ALK, ROS1, insulinlike growth factor-1 receptor (IGF-1R), and FLT-3, as well as EGFR deletion and point mutations
Brigatinib inhibited autophosphorylation of ALK and ALK-mediated phosphorylation of the downstream signaling proteins STAT3, AKT, ERK1/2, and S6 in in vitro and in vivo assays
Exhibited in vivo antitumor activity against 4 mutant forms of EML4-ALK, including G1202R and L1196M mutants identified in NSCLC tumors in patients who have progressed on crizotinib
Also reduced tumor burden and prolonged survival in mice implanted intracranially with an ALK-driven tumor cell line
Note
Trepmac 90 mg Tablet manufactured by Genvio Pharma Ltd.. Its generic name is Brigatinib. Trepmac is availble in Bangladesh.
Farmaco BD drug index information on Trepmac Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.