Generic Name: selpercatinib

Pronunciation: N/A

Abbreviation: N/A

Other Market Name: N/A

Drug Class: Targeted Therapy Medications

Company: Eli Lilly and Company

Approval Status: Approved

Generic Version Available: No

Experimental Code: LOXO-292

Drug Indication

Retevmo is a kinase inhibitor approved for the treatment of metastatic non-small-cell lung cancer and advanced or metastatic thyroid cancer with RET gene fusions or mutations.

General Info

Retevmo blocks the RET protein, which plays a role in cell proliferation. Mutations or fusions in the RET gene can lead to greater activity that drives the development of cancer. These RET alterations are rare overall, occurring in less that 1% of all cancers, but they are present in a majority of medullary thyroid tumors.

The LIBRETTO-001 trial showed that Retevmo led to complete or partial tumor shrinkage in 64% of previously treated adults with RET fusion-positive non-small-cell lung cancer, rising to 85% for those starting treatment for the first time. The overall response rate was 69% for treatment-experienced and 73% for previously untreated adults and adolescents with RET-mutant medullary thyroid tumors, and 79% and 100%, respectively, for those with RET fusion-positive thyroid cancer. Retevmo was first approved in May 2020.


Dosing Info:

Retevmo is taken as a capsule twice daily.

Side Effects

Common adverse reactions included diarrhea, constipation, dry mouth, fatigue, swelling, rash, high blood pressure, elevated ALT and AST liver enzymes, elevated glucose and cholesterol, and other lab test abnormalities. Potential serious side effects may include liver toxicity, severe high blood pressure, bleeding, heart rhythm abnormalities, hypersensitivity reactions and slow wound healing. Retevmo can cause fetal harm if used during pregnancy.

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Last Reviewed: May 10, 2020