drug · small molecule

RETEVMO

updated 3mo ago

by $LLY ELI LILLY & Co🔗 ChEMBL

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Small molecule drug with a maximum clinical stage of Approval (across all indications), with 11 approved and 2 investigational indications.

targets

Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RETProto-oncogene tyrosine-protein kinase receptor RetKinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET

all catalysts(0)

nothing on the calendar yet

Trials studying RETEVMO

phase2A Study of Selpercatinib (LY3527723) in Participants With Advanced Solid Tumors Including RET Fusion-positive Solid Tumors, Medullary Thyroid Cancer and Other Tumors With RET Activationactive not recruitingn=77
phase2Selpercatinib Pre-RAI in Patients With RET Fusion Thyroid Cancer (RAISE)recruitingn=13
phase3A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Canceractive not recruitingn=291
phase3A Study of Selpercatinib After Surgery or Radiation in Participants With Non-Small Cell Lung Cancer (NSCLC)active not recruitingn=152
phase2A Study of Oral LOXO-292 (Selpercatinib) in Pediatric Participants With Advanced Solid or Primary Central Nervous System (CNS) Tumorsactive not recruitingn=36
phase1A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participantscompletedn=16
phase3A Study of Selpercatinib (LY3527723) in Participants With Advanced or Metastatic RET Fusion-Positive Non-Small Cell Lung Canceractive not recruitingn=261
phase1A Study of Effects of Selpercatinib (LY3527723) on Midazolam in Healthy Participantscompletedn=16

more trials →

News(2)

OncLive Polls Reveal Picks for Top Lung Cancer Abstracts at ASCO 2026
Lung cancer experts rank key abstracts of interest from the upcoming ASCO Annual Meeting on OncLive’s social media.
onclive · 3mo ago
Track the Lung Cancer Abstracts That are Gaining Attention at ASCO 2026
Read on to see what data are poised to shape clinical discussions and decision-making in lung cancer at 2026 ASCO Annual Meeting in Chicago, Illinois.
onclive · 3mo ago

brand

RETEVMO

trade names

Retevmo, Retsevmo

generic

SELPERCATINIB

MOA

12.1 Mechanism of Action Selpercatinib is a kinase inhibitor. Selpercatinib inhibited wild-type RET and multiple mutated RET isoforms as well as VEGFR1 and VEGFR3 with IC 50 values ranging from 0.92 nM to 67.8 nM. In other enzyme assays, selpercatinib also inhibited FGFR 1, 2, and 3 at higher concentrations that were still clinically achievable. In cellular assays, selpercatinib inhibited RET at approximately 60-fold lower concentrations than FGFR1 and 2 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, RET V804M, and RET M918T. In addition, selpercatinib showed anti-tumor activity in mice intracranially implanted with a patient-derived RET fusion positive tumor.

indication

1 INDICATIONS AND USAGE RETEVMO ® is a kinase inhibitor indicated for the treatment of: Adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test ( 1.1 ) Adult and pediatric patients 2 years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved test, who require systemic therapy ( 1.2 ) Adult and pediatric patients 2 years of age and older with advanced or metastatic thyroid cancer with a RET gene fusion, as detected by an FDA-approved test, who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate) ( 1.3 ) Adult and pediatric patients 2 years of age and older with locally advanced or metastatic solid tumors with a RET gene fusion, as detected by an FDA-approved test, that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options 1 ( 1.4 ) 1 This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s). 1.1 RET Fusion-Positive Non-Small Cell Lung Cancer RETEVMO ® is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test. 1.2 RET -Mutant Medullary Thyroid Cancer RETEVMO is indicated for the treatment of adult and pediatric patients 2 years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved test, who require systemic therapy. 1.3 RET Fusion-Positive Thyroid Cancer RETEVMO is indicated for the treatment of adult and pediatric patients 2 years of age and older wi

Data sources

ClinicalTrials.gov · OpenTargets

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News(2)

OncLive Polls Reveal Picks for Top Lung Cancer Abstracts at ASCO 2026

Lung cancer experts rank key abstracts of interest from the upcoming ASCO Annual Meeting on OncLive’s social media.

onclive · 3mo ago

Track the Lung Cancer Abstracts That are Gaining Attention at ASCO 2026

Read on to see what data are poised to shape clinical discussions and decision-making in lung cancer at 2026 ASCO Annual Meeting in Chicago, Illinois.

onclive · 3mo ago

RETEVMO

🐶 often sniffed alongside

targets

all catalysts(0)

Trials studying RETEVMO

News(2)

Report a data issue

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RETEVMO

🐶 often sniffed alongside

targets

all catalysts(0)

Trials studying RETEVMO

News(2)

Report a data issue

comments(0)