# Selpercatinib

Source: https://onco.cc/drugs/selpercatinib/  
OnCo record `selpercatinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Selpercatinib is a selective RET inhibitor approved for any tumour with a RET fusion, with a further label update in July 2026.

## Summary

Selpercatinib is a selective RET kinase inhibitor, designed to avoid the off-target VEGFR effects of older multikinase drugs, taken as 160 mg twice daily. LIBRETTO-001 showed a response rate of about 84% in treatment-naive RET-fusion NSCLC, LIBRETTO-431 beat chemo-immunotherapy first line, and LIBRETTO-531 beat cabozantinib or vandetanib in RET-mutant medullary thyroid cancer. It was approved in 2020 for RET-fusion NSCLC and thyroid cancer and RET-mutant MTC, gained a tumour-agnostic RET-fusion indication in 2022, and a July 2026 FDA action is listed among that month's oncology approvals. Hypertension, raised transaminases and QT prolongation are the main adverse events. Acquired resistance through RET solvent-front mutations and bypass pathways is the current limit. For a newcomer: a pill that works wherever a RET fusion drives the cancer, regardless of organ.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-04
- Brand: Retevmo
- Modality: Small-molecule kinase inhibitor (RET)
- Mechanism: Highly selective RET TKI.
- Approvals: US 2020: RET-fusion NSCLC and thyroid; RET-mutant MTC; US 2022: RET-fusion solid tumours (tumour-agnostic); US 2026: Label update (July 2026); EU 2021: EU brand Retsevmo; England (NICE) 2023: Untreated RET fusion-positive advanced non-small-cell lung cancer; England (NICE) 2025: Previously treated RET fusion-positive advanced non-small-cell lung cancer not previously treated with a RET inhibitor
- Dosing: Oral; 160 mg twice daily (≥50 kg); 120 mg BID (<50 kg); paediatric by BSA

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Selpercatinib
- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Selpercatinib
- NICE TA911: selpercatinib for untreated RET fusion-positive advanced non-small-cell lung cancer: https://www.nice.org.uk/guidance/ta911
- NICE TA1042: selpercatinib for previously treated RET fusion-positive advanced non-small-cell lung cancer: https://www.nice.org.uk/guidance/ta1042

## Connected records

- biomarkers: [RET fusion and RET mutation](https://onco.cc/biomarkers/ret-fusion/)
- cancers: [Colorectal cancer](https://onco.cc/cancers/colorectal/), [Lung cancer (all types)](https://onco.cc/cancers/lung-cancer/), [Medullary thyroid cancer](https://onco.cc/cancers/medullary-thyroid-cancer/), [Metastatic cancer (cancer that has spread)](https://onco.cc/cancers/metastatic-cancer/), [Multiple endocrine neoplasia syndromes (MEN1, MEN2, MEN4)](https://onco.cc/cancers/multiple-endocrine-neoplasia/), [Multiple endocrine neoplasia type 2 (MEN2A and MEN2B)](https://onco.cc/cancers/men2-syndrome/), [Non-small-cell lung cancer](https://onco.cc/cancers/nsclc/), [Papillary thyroid cancer](https://onco.cc/cancers/papillary-thyroid-cancer/), [RET fusion-positive non-small-cell lung cancer](https://onco.cc/cancers/ret-fusion-nsclc/), [Thyroid cancer](https://onco.cc/cancers/thyroid/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/), [Thyroglobulin, calcitonin and CEA in thyroid cancer follow-up](https://onco.cc/technologies/thyroid-cancer-markers/)
- targets: [RET](https://onco.cc/targets/ret/)
- companies: [Eli Lilly (incl. Loxo)](https://onco.cc/companies/eli-lilly/)
- terms: [Cancer Drugs Fund (England)](https://onco.cc/terms/cancer-drugs-fund/), [Lung cancer drugs in England: what NICE has recommended](https://onco.cc/terms/lung-uk-drug-access/), [RACE for Children Act](https://onco.cc/terms/race-for-children-act/), [Tumour-agnostic (tissue-agnostic) approval](https://onco.cc/terms/tumour-agnostic/)
- trials: [A Study of Oral LOXO-292 (Selpercatinib) in Pediatric Participants With Advanced Solid or Primary Central Nervous System (CNS) Tumors](https://onco.cc/trials/nct03899792/), [A Study of Selpercatinib (LOXO-292) in Participants With Advanced Solid Tumors, RET Fusion-Positive Solid Tumors, and Medullary Thyroid Cancer (LIBRET](https://onco.cc/trials/nct03157128/), [A Study of Selpercatinib (LY3527723) in Participants With Advanced Solid Tumors Including RET Fusion-positive Solid Tumors, Medullary Thyroid Cancer a](https://onco.cc/trials/nct04280081/), [A Study of Selpercatinib After Surgery or Radiation in Participants With Non-Small Cell Lung Cancer (NSCLC)](https://onco.cc/trials/nct04819100/), [LIBRETTO-431](https://onco.cc/trials/libretto-431/), [LIBRETTO-531](https://onco.cc/trials/libretto-531/), [NCI-COG Pediatric MATCH (APEC1621)](https://onco.cc/trials/pediatric-match/)
- drugs: [Pralsetinib](https://onco.cc/drugs/pralsetinib/)
- pairings: [Sequence: targeted therapy before immunotherapy in driver-positive NSCLC](https://onco.cc/pairings/targeted-before-io-nsclc/)
- people: [Alexander Drilon](https://onco.cc/people/alexander-drilon/), [Koichi Goto](https://onco.cc/people/goto-koichi/), [Lori J. Wirth](https://onco.cc/people/lori-wirth/)
- bottlenecks: [Rare and paediatric cancers without markets](https://onco.cc/bottlenecks/b-rare-cancers/)
- key papers: [LIBRETTO-001: selpercatinib in RET fusion-positive non-small-cell lung cancer](https://onco.cc/key-papers/paper-libretto-001-selpercatinib-nsclc-nejm-2020/), [LIBRETTO-431: first-line selpercatinib versus chemotherapy with or without pembrolizumab in RET fusion-positive lung cancer](https://onco.cc/key-papers/paper-libretto-431-nejm-2023/), [LIBRETTO-531: selpercatinib versus cabozantinib or vandetanib in advanced RET-mutant medullary thyroid cancer](https://onco.cc/key-papers/paper-libretto-531-nejm-2023/)
- pathways: [Non-small cell lung cancer (KEGG map)](https://onco.cc/pathways/nsclc-signalling/), [Receptor tyrosine kinase activation](https://onco.cc/pathways/rtk-activation/), [Thyroid cancer (KEGG map)](https://onco.cc/pathways/thyroid-cancer-signalling/)
- roadmaps: [Targeted therapy roadmap: imatinib → designed for resistance → the undruggable drivers fall](https://onco.cc/roadmaps/targeted-therapy-roadmap/)

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