ROS1-positive NSCLC: Adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer. NTRK gene fusion-positive solid tumors: Adult patients with locally advanced or metastatic solid tumors with a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, who have no satisfactory alternative treatments or whose cancer has progressed following treatment.
Weeks 1–2: 160 mg orally once daily. Week 3 onwards: 160 mg orally twice daily. Take with or without food. Swallow capsules whole.
Dose reduction: First reduction to 160 mg once daily; second to 120 mg once daily. Discontinue if unable to tolerate 120 mg once daily.
Capsules: 40 mg, 160 mg
None established in prescribing information.
Dizziness (45%), Dysgeusia (43%), Peripheral Neuropathy (38%), Constipation (33%), Cognitive Impairment (33%), Fatigue (31%), Dyspnea (27%), Ataxia (26%)
Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.
Strong CYP3A4 inhibitors: Avoid; if unavoidable, reduce repotrectinib dose.
Strong CYP3A4 inducers: Avoid concomitant use.
Sensitive CYP3A4 substrates with narrow therapeutic index: Avoid concomitant use.
Can cause fetal harm. Advise females of reproductive potential to use effective contraception. Consult the full prescribing information for pregnancy risk details.
Advise women not to breastfeed during treatment and for a period after the last dose. Refer to prescribing information for duration guidance.
Safety and effectiveness in pediatric patients have not been established unless otherwise noted in the full prescribing information.
Dose modifications for organ impairment are specified in the complete prescribing information.
Repotrectinib is a next-generation ROS1 and TRK (TRKA/B/C) tyrosine kinase inhibitor engineered with a compact macrocyclic structure to address acquired resistance mutations (e.g., ROS1 G2032R, NTRK XDFG mutations) that limit earlier-generation TKIs. It competitively inhibits ATP binding in the kinase domain, blocking downstream proliferative signaling.
Tmax: ~4 hours. Protein binding: ~98%. Hepatic metabolism via CYP3A4. Half-life: ~35 hours. Elimination: feces (83%), urine (7%). Steady state: ~14 days.
Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.
Augtyro has FDA-approved indications across the following cancer types covered on CancerDrugEvidence:
Augtyro (repotrectinib) is an FDA-approved oncology agent. Refer to the full prescribing information for complete indication details.
Refer to the full prescribing information for dosing schedules, administration instructions, and dose modifications.
Repotrectinib is a next-generation ROS1 and TRK (TRKA/B/C) tyrosine kinase inhibitor engineered with a compact macrocyclic structure to address acquired resistance mutations (e.g., ROS1 G2032R, NTRK XDFG mutations) that limit earlier-generation TKIs. It competitively inhibits ATP binding in the kina
Dizziness (45%), Dysgeusia (43%), Peripheral Neuropathy (38%), Constipation (33%), Cognitive Impairment (33%), Fatigue (31%), Dyspnea (27%), Ataxia (26%)