Overview
Selpercatinib is a kinase inhibitor with enhanced specificity for RET tyrosine kinase receptors (RTKs) over other RTK classes. Enhanced RET (Rearranged during transfection) oncogene expression is a hallmark of many cancers. Although multikinase inhibitors, including cabozantinib, ponatinib, sorafenib, sunitinib, and vandetanib, have shown efficacy in RET-driven cancers, their lack of specificity is generally associated with substantial toxicity. Selpercatinib (LOXO-292) and pralsetinib (BLU-667) represent the first generation of specific RET RTK inhibitors for the treatment of RET-driven cancers. Although selpercatinib is currently still under investigation in clinical trial NCT04211337, it was granted accelerated FDA approval on May 8, 2020, for specific RET-driven cancer indications. It is currently marketed under the brand name RETEVMO™ by Loxo Oncology Inc. Selpercatinib is also approved by the European Commission.
Indication
Selpercatinib is approved to treat: Selpercatinib is currently approved for these indications under an accelerated approval scheme and continued approval may be contingent on future confirmatory trials.
Associated Conditions
- Locally Advanced Solid Neoplasm
- Metastatic Solid Neoplasm
- Advanced RET-fusion thyroid cancer
- Advanced RET-mutant medullary thyroid cancer
- Metastatic RET-fusion Non Small Cell Lung Cancer
- Metastatic RET-fusion thyroid cancer
- Metastatic RET-mutant medullary thyroid cancer
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/06/08 | Phase 4 | Not yet recruiting | Fujian Medical University | ||
2024/08/01 | N/A | Recruiting | |||
2024/06/13 | Phase 2 | Recruiting | |||
2023/06/18 | Phase 1 | Completed | |||
2022/12/30 | Phase 2 | Recruiting | |||
2022/11/29 | Phase 1 | Completed | |||
2022/11/29 | Phase 1 | Completed | |||
2022/07/21 | Phase 1 | Completed | |||
2022/07/21 | Phase 1 | Completed | |||
2022/07/21 | Phase 1 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Eli Lilly and Company | 0002-3977 | ORAL | 40 mg in 1 1 | 9/21/2022 | |
| Eli Lilly and Company | 0002-2980 | ORAL | 80 mg in 1 1 | 9/21/2022 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 2/11/2021 | ||
Authorised | 2/11/2021 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| TANSTRIVE HARD CAPSULES 40MG | SIN16990P | CAPSULE | 40.0mg | 4/24/2024 | |
| TANSTRIVE HARD CAPSULES 80MG | SIN16991P | CAPSULE | 80.0mg | 4/24/2024 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Selpercatinib Capsules | 国药准字HJ20220077 | 化学药品 | 胶囊剂 | 9/30/2022 | |
| Selpercatinib Capsules | 国药准字HJ20220078 | 化学药品 | 胶囊剂 | 9/30/2022 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| RETEVMO selpercatinib 40 mg immediate release capsules | 391331 | Medicine | A | 7/3/2023 | |
| RETEVMO selpercatinib 80 mg immediate release capsules | 391330 | Medicine | A | 7/3/2023 |
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