Drug · Small Molecule

Selpercatinib

CI-DRUG-00000547Explore in graph →NCIt C134987 CHEMBL4559134 CIViC Approved

Regulatory

Approvals (26)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

health-canada-dpdRegulatory26 approval records from 3 sources (hover a row badge for its dataset) · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
CA Health Canada	—	Marketed in Canada as RETEVMO (DIN 02565676) under ATC L01EX22 SELPERCATINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Aug 4, 2026	health-canada-dpd
CA

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 18 hours agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	16	2	3	18	26	CA, EU, US	May 8, 2020	2016-08
Malignant Lung Neoplasm	Approved	Phase 4	6	0	2	8	2	US	May 8, 2020	May 2, 2017
Malignant Thyroid Gland Neoplasm	Approved	Phase 3	6	1	1	6	4	US	May 8, 2020	May 2, 2017
Malignant Central Nervous System Neoplasm	Phase2	Phase 2	2	0	0

Curated evidence

Clinical evidence (43)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–43 of 43 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
RET Fusion3
Selpercatinib	Lung Non-Small Cell Carcinoma

Clinical trials

Trials with this intervention (21)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–21 of 21 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT07822880	A Study of Selpercatinib (LY3527723) in Participants With Rearranged During Transfection (RET)-Altered Cancers in India	not yet recruiting	Phase 4	30	Eli Lilly and CompanyINDUSTRY	1	Sep 23, 2026	clinicaltrials
NCT04280081	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

Molecule

Record

Kind: Small Molecule
Mechanism: Tyrosine-protein kinase receptor RET inhibitor; Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET inhibitor; Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET inhibitor
Targets: 3 genes
UNII: CEGM9YBNGD
Aliases: 6-(2-Hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo(3.1.1)heptan-3-yl)pyridin-3-yl)pyrazolo(1,5-a)pyridine-3-carbonitril, 6-(2-Hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo(3.1.1)heptan-3-yl)pyridin-3-yl)pyrazolo(1,5-a)pyridine-3-carbonitrile, LOXO 292, LOXO-292, LOXO292, LY-3527723, LY3527723, Retevmo, RETEVMO, RET Inhibitor LOXO-292, RET Kinase Inhibitor LOXO-292, Retsevmo, Selpercatinib, WHO 10967

Data updated 21 hours agoSource updated unknown

Identifiers

Codes (10)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EX22	SELPERCATINIB
DIN (Health Canada)

RET Fusion8
Selpercatinib	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	A	Supports Sensitivity Response	4	submitted	EID11318 In a follow up publication on the NCT03157128 clinical trial, results of 316 RET fusion positive NSCLC patients treated with the RET inhibitor selpercatinib were reported. Of note, this includes 144 … (full text at CIViC) PMID 36122315 · Drilon et al., 2023 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID7066 In this phase 1 trial, 57 patients with RET fusion- or mutation positive cancers were treated in 7 dose levels. Among patients with RET-Fusion positive NSCLC, objective response rates were 65% (n = 17… (full text at CIViC) Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	4	accepted	EID8850 Patients with RET-fusion positive non-small cell lung cancer were enrolled in this phase 1-2 trial of RET inhibitor selpercatinib. Among 105 consecutively enrolled patients who had previously received… (full text at CIViC) PMID 32846060 · Drilon et al., 2020 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	3	submitted	EID12135 In this arm of the trial (NCT03157128), the intracranial objective response rate (iORR) was assessed in 80 patients with RET fusion-positive non-small cell lung cancer (NSCLC) treated with selpercatin… (full text at CIViC) PMID 34088726 · Subbiah et al., 2021 · Open in CIViC	civic
〃	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID6949 In a preclinical analysis, RET inhibitor LOXO-292 was active against RET-Fusion positive cell lines and xenograft models PMID 29912274 · Subbiah et al., 2018 · Open in CIViC	civic
〃	Malignant Thyroid Gland Neoplasm	Predictive	A	Supports Sensitivity Response	4	accepted	EID8852 In this phase 1/2 trial (NCT03157128), patients with RET altered thyroid cancers were enrolled to receive the highly selective RET inhibitor selpercatinib. Among 19 patients with previously treated RE… (full text at CIViC) PMID 32846061 · Wirth et al., 2020 · Open in CIViC	civic
〃	Solid NeoplasmCURATED_BROADER	Predictive	B	Supports Sensitivity Response	3	submitted	EID12134 In this arm of the trial (LIBRETTO-001), the efficacy of selpercatinib was tested in 45 patients harbouring RET fusion-positive solid tumours (excluding lung or thyroid tumours). The objective respons… (full text at CIViC) PMID 36108661 · Subbiah et al., 2022 · Open in CIViC	civic
〃	Thyroid Gland Papillary CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	4	accepted	EID7069 In this phase 1 trial, patients with RET-fusion or mutation positive cancers were treated with the selective RET-inhibitor selpercatinib (LOXO-292). Among the 6 patients with RET-fusion positive papil… (full text at CIViC) Open in CIViC	civic

RET E632_L633del5
Selpercatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID12712 Ba/F3 cells transformed with E632_L633del showed IL-3 independent growth. Selpercatinib inhibited growth of the cells at approximately 16 nM. This was 4-5 fold higher than the IC50 for RET M918T cells… (full text at CIViC) PMID 37376747 · Szymczak et al., 2023 · Open in CIViC	civic
Pralsetinib + SelpercatinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Resistance	2	submitted	EID12715 Wildtype or 632_633del RET was expressed in HEK293 cells, and MAPK reporter response assays were performed on these cells in triplicate, at various concentrations of inhibitors including selpercatinib… (full text at CIViC) PMID 36416226 · Wijewardene et al., 2023 · Open in CIViC	civic
Selpercatinib	Thyroid Gland Medullary CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	3	accepted	EID11875 Among 319 medullary thyroid cancer patients enrolled in the LIBRETTO-001 trial, 9 patients harbored the RET p.E632_L633del mutation (c.1894_1899delGAGCTG) in their tumor. After treatment with the sel… (full text at CIViC) PMID 37376747 · Szymczak et al., 2023 · Open in CIViC	civic
〃	Thyroid Gland Medullary CarcinomaALIAS	Predictive	C	Does Not Support Sensitivity Response	2	submitted	EID12714 A 35 yr old man presented with a 9 month history of worsening right side flank pain and no significant family history. Calcitonin was elevated. After imaging, total thyroidectomy with modified radica… (full text at CIViC) PMID 36416226 · Wijewardene et al., 2023 · Open in CIViC	civic
〃	Thyroid Gland Medullary CarcinomaALIAS	Predictive	C	Supports Sensitivity Response	3	submitted	EID12716 A patient with advanced progressive medullary thyroid cancer and distant metastatic disease harbored the somatic RET E632_L633del indel and was treated under the LIBRETTO-201 (NCT03906331) trial. Selp… (full text at CIViC) PMID 35616103 · Elisei et al., 2022 · Open in CIViC	civic

RET M918T4
Pralsetinib + SelpercatinibSubstitutes	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	4	accepted	EID11867 Ba/F3 transformed cells harboring RET D898_E901del, T930K, T930P, or M918T mutations were shown to be sensitive to the highly selective RET inhibitors selpercatinib (LOXO-292) and pralsetinib (BLU-667… (full text at CIViC) PMID 32284345 · Zhao et al., 2020 · Open in CIViC	civic
Selpercatinib	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	2	accepted	EID11876 Preclinical data demonstrated Ba/F3 cells transformed with RET p.M918T were sensitive to selpercatinib with an IC50 of 5nM. M918T was included as a positive control for other variants that were being … (full text at CIViC) PMID 37376747 · Szymczak et al., 2023 · Open in CIViC	civic
〃	Thyroid Gland Medullary CarcinomaALIAS	Predictive	A	Supports Sensitivity Response	5	accepted	EID12598 The Phase 3 trial for the selective and brain-penetrant RET kinase inhibitor selpercatinib in Medullary Thyroid Cancer (MTC) LIBRETTO-531 (NCT04211337) consisted of 291 total patients. The patients … (full text at CIViC) PMID 37870969 · Hadoux et al., 2023 · Open in CIViC	civic
〃	Thyroid Gland Medullary CarcinomaALIAS	Predictive	C	Supports Sensitivity Response	4	rejected	EID11306 After progressing on 6 multi-kinase inhibitor (MKI) regimens (including sorafenib , vandetanib, cabozantinib, MGCD-516, RXDX-105, and vandetanib plus everolimus ), a metastatic medullary thyroid cance… (full text at CIViC) PMID 29912274 · Subbiah et al., 2018 · Open in CIViC	civic

RET Mutation + RET Fusion3
Selpercatinib	Malignant Thyroid Gland Neoplasm	Predictive	A	Supports Sensitivity Response	4	rejected	EID11268 In this phase 1/2 study, 55 patients with RET-mutant medullary thyroid cancer who had previously received vandetanib and/or cabozantinib, 88 patients with the same disease who had not previously recei… (full text at CIViC) PMID 32846061 · Wirth et al., 2020 · Open in CIViC	civic
〃	Solid NeoplasmCURATED_BROADER	Predictive	A	Supports Sensitivity Response	4	accepted	EID12056 As part of this trial, 27 pediatric patients (aged 2-20), harbouring, RET-mutant medullary thyroid cancer (MTC, n = 14), RET fusion-positive papillary thyroid cancer (RTC, n=10), or other tumour types… (full text at CIViC) Open in CIViC	civic
〃	Solid NeoplasmCURATED_BROADER	Predictive	A	Supports Sensitivity Response	5	accepted	EID12708 In the phase 1/2 trial LIBRETTO-121 (NCT03899792), for patients 0.5-21 yrs old with advanced RET-altered solid tumors, dosing started at 92 mg/m2 twice a day of Selpercatinib. Patients had RET-mutant… (full text at CIViC) Open in CIViC	civic

RET M918T + RET V804M2
Selpercatinib	Thyroid Gland Medullary CarcinomaALIAS	Predictive	C	Supports Sensitivity Response	4	accepted	EID6950 After progressing on 6 multi-kinase inhibitor (MKI) regimens (including sorafenib , vandetanib, cabozantinib, MGCD-516, RXDX-105, and vandetanib plus everolimus ), a metastatic medullary thyroid cance… (full text at CIViC) PMID 29912274 · Subbiah et al., 2018 · Open in CIViC	civic
〃	Thyroid Gland Medullary CarcinomaALIAS	Predictive	C	Supports Sensitivity Response	4	rejected	EID11307 After progressing on 6 multi-kinase inhibitor (MKI) regimens (including sorafenib , vandetanib, cabozantinib, MGCD-516, RXDX-105, and vandetanib plus everolimus ), a metastatic medullary thyroid cance… (full text at CIViC) PMID 29912274 · Subbiah et al., 2018 · Open in CIViC	civic