Last reviewed 2026-04-20 · How we verify

Augtyro (REPOTRECTINIB)

Augtyro blocks the activity of ROS1 and NTRK kinases, which are abnormal proteins that help cancer cells grow and spread.

Augtyro (repotrectinib) is a small molecule kinase inhibitor developed by Bristol, approved in 2023 for the treatment of locally advanced or metastatic ROS1-positive non-small cell lung cancer and NTRK gene fusion-positive solid tumors. It works by selectively inhibiting the activity of ROS1 and NTRK kinases, which are involved in the growth and spread of cancer cells. Augtyro is a patented medication with no generic manufacturers available. Key safety considerations include potential side effects such as fatigue, nausea, and liver enzyme elevations. Augtyro's commercial status and pharmacokinetic properties, including half-life and bioavailability, are not publicly disclosed.

At a glance

Mechanism of action

Repotrectinib is an inhibitor of proto-oncogene tyrosine-protein kinase ROS1 (ROS1) and of the tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC. Fusion proteins that include ROS1 or TRK domains can drive tumorigenic potential through hyperactivation of downstream signaling pathways leading to unconstrained cell proliferation. Repotrectinib exhibited anti-tumor activity in cultured cells expressing ROS1 fusions and mutations including SDC4-ROS1, SDC4-ROS1 G2032R , CD74-ROS1, CD74-ROS1 G2032R , CD74-ROS1 D2033N , and CD74-ROS1 L2026M . Repotrectinib also inhibited cell proliferation in cultured cells expressing NTRK fusions and mutations including LMNA-TRKA, LMNA-TRKA G595R , EVT6-TRKB G639R , and ETV6-TRKC G623R .

Approved indications

• Locally advanced or metastatic ROS1-positive non-small cell lung cancer
• NTRK gene fusion-positive solid tumors

Common side effects

• Dizziness
• Dysgeusia
• Peripheral neuropathy
• Ataxia
• Cognitive impairment
• Dyspnea
• Fatigue
• Constipation
• Nausea
• Muscular weakness
• Pneumonia
• Headache

Drug interactions

• Strong and Moderate CYP3A Inhibitors
• P-gp inhibitors
• Strong and Moderate CYP3A Inducers
• Certain CYP3A Substrates
• Hormonal contraceptives
• CYP3A4 Substrates
• CYP3A4 Substrates
• CYP3A4 Substrates
• CYP3A4 Substrates
• CYP3A4 Substrates
• CYP3A4 Substrates
• CYP3A4 Substrates

Key clinical trials

• Study to Evaluate the Effect of Repotrectinib on the Drug Levels of Transporter and CYP P450 Probe Substrates in Healthy Adult Participants (PHASE1)
• Phase II Efficacy Study of Repotrectinib in Frail and/or Elderly Patients With ROS1-rearranged Advanced NSCLC (PHASE2)
• A Study of Repotrectinib in Combination With Chemotherapy in Children and Young Adults With Solid Tumor Cancer (PHASE1,PHASE2)
• REPotrectinib in ROS1-positive Non-small Cell Lung Cancer Patients With Active Brain mEtastasis (PHASE2)
• Phase II Study of REPotrectinib With or Without Fulvestrant in Patients With Hormone Receptor-positive Human Epidermal Growth Factor 2-negative Metastatic Invasive LObular Carcinoma Who Received a Prior Endocrine Therapy in Combination With Cyclin-dependent Kinase 4 and 6 Inhibitor (REPLOT Trial) (PHASE2)
• A Study of Repotrectinib Versus Crizotinib in Participants With Locally Advanced or Metastatic Tyrosine Kinase Inhibitor (TKI)-naïve ROS1-positive Non-Small Cell Lung Cancer (NSCLC) (TRIDENT-3) (PHASE3)
• A Study of Repotrectinib in Pediatric and Young Adult Subjects Harboring ALK, ROS1, OR NTRK1-3 Alterations (PHASE1,PHASE2)
• A Study to Assess the Drug Levels of Repotrectinib in Healthy Participants and Participants With Moderate and Severe Hepatic Impairment (PHASE1)

Patents

Primary sources

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