General Information

Augtyro (repotrectinib) is a kinase inhibitor.

Augtryo is specifically indicated for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC).

Dosing/Administration

Augtryo is supplied as capsules for oral administration. 

Select patients for the treatment of locally advanced or metastatic NSCLC with Augtryo based on the presence of ROS1 rearrangement(s) in tumor specimens.

Prior to initiating Augtry, discontinue strong and moderate CYP3A inhibitors for 3 to 5 elimination half-lives of the CYP3A inhibitor

Prior to initiation of Augtryo evaluate liver function tests including bilirubin and uric acid level 

The recommended dosage of Augtryo is 160 mg taken orally once daily with or without food for 14 days, then increase to 160 mg twice daily and continue until disease progression or unacceptable toxicity.

Mechanism of Action

Augtyro (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 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.

Side Effects

Adverse effects associated with the use of Augtryo may include, but are not limited to, the following:

• dizziness
• dysgeusia
• peripheral neuropathy
• constipation
• dyspnea
• ataxia
• fatigue
• cognitive disorders
• muscular weakness

Clinical Trial Results

The FDA approval of Augtryo was based on the TRIDENT-1 study, an open-label, single-arm, Phase 1/2 trial that evaluated Augtryo  in TKI-naïve and TKI-pretreated patients. In TKI-naïve patients (n=71), the primary endpoint of objective response rate (ORR), defined as the percentage of people treated within a certain period of time whose tumor size decreased (partial response) or who no longer have signs of cancer (complete response), was 79%. The median duration of response (mDOR) was 34.1 months. Among patients pretreated with one prior ROS1 TKI and no prior chemotherapy (n=56), the ORR was 38% and the mDOR was 14.8 months. Among those who had measurable central nervous system (CNS) metastases at baseline, responses in intracranial lesions were observed in 7 of 8 TKI-naïve patients (n=71) and 5 of 12 of those who were TKI-pretreated (n=56).