Drugs / Selpercatinib
last change Jul 2026 re-read 2 minutes ago

Selpercatinib

Small molecule targets RET via inhibition

Developed for
non-small cell lung carcinoma · medullary thyroid gland carcinoma · thyroid gland papillary carcinoma · breast cancer · colon carcinoma · ependymoma · Ewing sarcoma · hepatoblastoma
+29 more · Langerhans cell histiocytosis · malignant germ cell tumor · malignant glioma · medulloblastoma · neuroblastoma · non-Hodgkin lymphoma · peripheral primitive neuroectodermal tumor · rhabdoid tumor · rhabdomyosarcoma · Wilms tumor · cancer · childhood malignant neoplasm · conventional osteosarcoma · differentiated thyroid carcinoma · digestive system cancer · fibrosarcoma · histiocytic sarcoma · infantile myofibromatosis · juvenile xanthogranuloma · malignant pancreatic neoplasm · metastatic malignant neoplasm · osteosarcoma · poorly differentiated thyroid gland carcinoma · primary organ-specific lymphoma · RET fusion positive cancer · thyroid gland follicular carcinoma · thyroid gland squamous cell carcinoma · thyroid gland undifferentiated (anaplastic) carcinoma · thyroid tumor
Investigated by
Eli Lilly and Company · Loxo Oncology, Inc. · National Cancer Institute (NCI) · AstraZeneca · SWOG Cancer Research Network · Amgen
+67 more · Bayer · Boehringer Ingelheim · Bristol-Myers Squibb · Changhai Hospital · Children's Hospital of Philadelphia · Children's Oncology Group · Clovis Oncology - Pharma and · Dalian Friendship Hospital Affiliated to Dalian Medical University · Dutch Cancer Society · Eisai Inc. · Fondazione per la Medicina Personalizzata · Fudan University · Fujian Cancer Hospital · Fujian Medical University · GlaxoSmithKline · Haukeland University Hospital · Helse Fonna · Helse Forde · Helse Møre og Romsdal HF · Helse Nord-Trøndelag HF · Helse Stavanger HF · Henan Cancer Hospital · Hospital of Southern Norway Trust · Hunan Provincial People's Hospital · Incyte Corporation · Innlandet Hospital Trust · Ipsen · Janssen, LP · Jiangsu Cancer Institute & Hospital · Liaoning Cancer Hospital & Institute · Lovisenberg Diakonale Hospital · M.D. Anderson Cancer Center · Massachusetts General Hospital · Merck Sharp & Dohme LLC · Nordland Hospital · Novartis · Oslo University Hospital · Ostfold Hospital Trust · Peking Union Medical College Hospital · Pfizer · Presbyterian Health Foundation · Roche Pharma AG · Ruijin Hospital · Shanghai 10th People's Hospital · Shanghai 6th People's Hospital · Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine · Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University · Shanxi Province Cancer Hospital · Sir Run Run Shaw Hospital · St. Olavs Hospital · Stelvio for Life · Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University · Sun Yat-sen University · Sykehuset Telemark · The Affiliated Hospital of Inner Mongolia Medical University · The First Affiliated Hospital of Anhui University of Chinese Medicine · The Hospital of Vestfold · The Netherlands Cancer Institute · The Third Affiliated Hospital of Soochow University · Tianjin Medical University Cancer Institute and Hospital · Union Hospital, Tongji Medical College, Huazhong University of Science and Technology · United States Department of Defense · University Hospital of North Norway · University Hospital, Akershus · University of Oklahoma · Vestre Viken Hospital Trust · Zhejiang Cancer Hospital

Regulatory milestones approvals, filings & regulatory actions · 8 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansions (6) US (FDA) RETEVMO 2022-09-21 – 2026-07-14 fda.gov
Approved EU (EMA) Retsevmo 2021-02-11 europa.eu
Approved US (FDA) RETEVMO 2020-05-08 fda.gov

Trials 36 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 01 trial
Phase 0 NCT07146893 Feb 2026 → Feb 2027 expected University of Oklahoma Not yet recruiting No outcome recorded
Phase 115 trials
Phase 1 NCT05906836 Jul → Oct 2023 Eli Lilly and Company Completed No outcome recorded
Phase 1 NCT05324124 Apr → Jun 2022 Loxo Oncology, Inc. Completed No outcome recorded
Phase 1 NCT05136404 Dec 2021 → Mar 2022 Loxo Oncology, Inc. Completed No outcome recorded
Phase 1 NCT05089019 Oct 2021 → Jul 2022 Loxo Oncology, Inc. Completed No outcome recorded
Phase 1 NCT04782076 Mar → May 2021 Loxo Oncology, Inc. Completed No outcome recorded
Phase 1 NCT05338502 Jul → Sep 2019 Eli Lilly and Company Completed No outcome recorded
Phase 1 NCT05630274 Apr → Jun 2019 Eli Lilly and Company Completed No outcome recorded
Phase 1 NCT05338515 Feb → Mar 2019 Eli Lilly and Company Completed No outcome recorded
Phase 1 NCT05469113 Jan → Mar 2019 Eli Lilly and Company Completed No outcome recorded
Phase 1 NCT05469100 Dec 2018 → Aug 2019 impaired renal function disease Eli Lilly and Company Completed No outcome recorded
Phase 1/22 trials
Phase 1/2 NCT03899792 Jun 2019 → Nov 2024 overdue fibrosarcoma, infantile myofibromatosis, medullary thyroid gland carcinoma, thyroid gland papillary carcinoma Eli Lilly and Company Active not recruiting No outcome recorded
Phase 1/2 NCT03157128 May 2017 → Feb 2025 overdue colon carcinoma, medullary thyroid gland carcinoma, non-small cell lung carcinoma Eli Lilly and Company Active not recruiting No outcome recorded
Phase 212 trials
Phase 2 NCT06458036 Jul 2024 → Nov 2030 expected childhood malignant neoplasm, differentiated thyroid carcinoma Children's Hospital of Philadelphia Recruiting No outcome recorded
Phase 2 NCT05668962 Mar 2023 → Mar 2025 overdue thyroid gland follicular carcinoma, thyroid gland papillary carcinoma Massachusetts General Hospital Recruiting No outcome recorded
Phase 2 NCT05364645 Jul 2022 → Jun 2023 non-small cell lung carcinoma SWOG Cancer Research Network Withdrawn No outcome recorded
Phase 2 NCT04320888 May 2021 → Sep 2024 overdue Ewing sarcoma, Langerhans cell histiocytosis, Wilms tumor, ependymoma +10 National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT04817956 Apr 2021 → Mar 2040 expected metastatic malignant neoplasm Oslo University Hospital Recruiting No outcome recorded
Phase 2 NCT04759911 Feb 2021 → Nov 2027 expected medullary thyroid gland carcinoma, poorly differentiated thyroid gland carcinoma, thyroid gland papillary carcinoma, thyroid gland squamous cell carcinoma +1 M.D. Anderson Cancer Center Active not recruiting No outcome recorded
Phase 2 NCT04591431 Oct 2020 → Dec 2024 breast cancer, digestive system cancer, non-small cell lung carcinoma Fondazione per la Medicina Personalizzata Unknown No outcome recorded
Phase 2 NCT04268550 Apr 2020 → Dec 2026 expected non-small cell lung carcinoma SWOG Cancer Research Network Active not recruiting No outcome recorded
Phase 2 NCT04280081 Mar 2020 → Mar 2021 overdue medullary thyroid gland carcinoma Eli Lilly and Company Active not recruiting No outcome recorded
Phase 2 NCT03944772 Jun 2019 → May 2025 overdue non-small cell lung carcinoma AstraZeneca Active not recruiting No outcome recorded
Phase 33 trials
Phase 3 NCT04819100 Dec 2021 → Jan 2026 overdue non-small cell lung carcinoma Eli Lilly and Company Active not recruiting No outcome recorded
Phase 3 NCT04194944 Feb 2020 → May 2023 overdue non-small cell lung carcinoma Eli Lilly and Company Active not recruiting No outcome recorded
Phase 3 NCT04211337 Feb 2020 → May 2023 overdue medullary thyroid gland carcinoma Loxo Oncology, Inc. Active not recruiting No outcome recorded
Phase 42 trials
Phase 4 NCT07010393 Jul 2025 → Dec 2027 expected thyroid tumor Fujian Medical University Not yet recruiting No outcome recorded
Phase 4 NCT06195228 Jan 2020 → Dec 2026 expected Fudan University Recruiting No outcome recorded
Phase not stated1 trial
NCT03906331 RET fusion positive cancer, breast cancer, colon carcinoma, malignant pancreatic neoplasm +3 Eli Lilly and Company Approved for marketing No outcome recorded

Evidence & citations 10 cited values

Every value below carries the sentence it was read from. 39 sources stand behind the page.

FieldValueCited text
Known as Selpercatinib “This is an open-label, first-in-human study designed to evaluate the safety, tolerability, pharmacokinetics (PK) and preliminary anti-tumor activity of selpercatinib (also...” NCT03157128
35

SelpercatinibNCT04817956

NCT07146893

NCT04819100

NCT04759911

NCT04782076

NCT05469100

NCT03899792

NCT05338489

NCT05906836

NCT03155620

NCT05338502

NCT03906331

NCT05136404

NCT06195228

NCT04280081

NCT05668962

NCT05469113

NCT04194944

NCT05364645

NCT04320888

NCT04591431

NCT05630287

NCT05089019

NCT05468164

NCT05630274

NCT06458036

NCT05338476

NCT05436912

NCT02925234

NCT04211337

NCT04268550

NCT03944772

NCT05324124

NCT05338515

NCT07010393

Known as LOXO-292 “This is an open-label, first-in-human study designed to evaluate the safety, tolerability, pharmacokinetics (PK) and preliminary anti-tumor activity of selpercatinib (also...” NCT03157128
1

“A Phase 2 Study of Oral Selpercatinib (LOXO-292) in Patients With Advanced Solid Tumors, Including Rearranged in Transfection (RET) Fusion-Positive Solid Tumors, Medullary...” NCT04280081

Known as LY3527723 “A Study of Selpercatinib (LY3527723) in Participants With Advanced Solid Tumors Including RET Fusion-positive Solid Tumors, Medullary Thyroid Cancer and Other Tumors With RET Activation” NCT04280081
Known as Ret inhibitor loxo-292 ChEMBL registry synonym — accepted as the source's own label CHEMBL4559134
Known as Retevmo “Selpercatinib (also known by the brand name Retevmo®/Retsevmo®) is a new treatment available in multiple countries” PMID 35969032 Aug 2022
Known as Retsevmo “Selpercatinib (also known by the brand name Retevmo®/Retsevmo®) is a new treatment available in multiple countries” PMID 35969032 Aug 2022
Action Inhibit “a first-in-class, highly selective, and potent small molecule RET kinase inhibitor” PMID 38661071 Feb 2025
Modality Small molecule “a first-in-class, highly selective, and potent small molecule RET kinase inhibitor” PMID 38661071 Feb 2025
Route Oral “receive selpercatinib PO BID” NCT03155620
Target RET “a first-in-class, highly selective, and potent small molecule RET kinase inhibitor” PMID 38661071 Feb 2025