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Retevmo (SELPERCATINIB)

Eli Lilly · FDA-approved approved Small molecule Quality 69/100

Retevmo works by blocking the activity of the RET protein, which is involved in the growth and spread of cancer cells.

Retevmo (selpercatinib) is a small molecule kinase inhibitor developed by LOXO ONCOLOGY INC and currently owned by Eli Lilly And Co. It targets the proto-oncogene tyrosine-protein kinase receptor Ret, a protein involved in the growth and spread of certain types of cancer. Retevmo is approved to treat advanced RET fusion-positive non-small cell lung cancer, advanced RET fusion-positive thyroid cancer, medullary thyroid carcinoma, and metastatic non-small cell lung cancer. The drug has a half-life of 32 hours and is patented, with no generic manufacturers available. Key safety considerations include potential liver damage and gastrointestinal side effects.

At a glance

Generic nameSELPERCATINIB
SponsorEli Lilly
Drug classKinase Inhibitor [EPC]
TargetProto-oncogene tyrosine-protein kinase receptor Ret
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved
First approval2020
Annual revenue700

Mechanism of action

Selpercatinib is kinase inhibitor. Selpercatinib inhibited wild-type RET and multiple mutated RET isoforms as well as VEGFR1 and VEGFR3 with IC50 values ranging from 0.92 nM to 67.8 nM. In other enzyme assays, selpercatinib also inhibited FGFR 1, 2, and at higher concentrations that were still clinically achievable. In cellular assays, selpercatinib inhibited RET at approximately 60-fold lower concentrations than FGFR1 and and approximately 8-fold lower concentration than VEGFR3.Certain point mutations in RET or chromosomal rearrangements involving in-frame fusions of RET with various partners can result in constitutively activated chimeric RET fusion proteins that can act as oncogenic drivers by promoting cell proliferation of tumor cell lines. In in vitro and in vivo tumor models, selpercatinib demonstrated anti-tumor activity in cells harboring constitutive activation of RET proteins resulting from gene fusions and mutations, including CCDC6-RET, KIF5B-RET,

Approved indications

Common side effects

Key clinical trials

Patents

PatentExpiryType

Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity
SEC EDGARRevenue + earnings

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