Overview
Capmatinib is a small molecule kinase inhibitor targeted against c-Met (a.k.a. hepatocyte growth factor receptor [HGFR]), a receptor tyrosine kinase that, in healthy humans, activates signaling cascades involved in organ regeneration and tissue repair. Aberrant c-Met activation - via mutations, amplification, and/or overexpression - is known to occur in many types of cancer, and leads to overactivation of multiple downstream signaling pathways such as STAT3, PI3K/ATK, and RAS/MAPK. Mutations in MET have been detected in non-small cell lung cancer (NSCLC), and the prevalence of MET amplification in epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI)-naive patients with NSCLC has been reported to be 1.4% - 21%. This co-occurrence has made c-Met a desirable target in the treatment of NSCLC. Manufactured by Novartis and marketed under the brand name Tabrecta, capmatinib was granted accelerated approval by the FDA on May 6, 2020, for the treatment of NSCLC in patients whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping. The presence of the mutation must be confirmed by an FDA-approved test, such as the FoundationOne CDx assay (manufactured by Foundation Medicine, Inc.), which was approved by the FDA on the same day. As this indication was granted under an accelerated approval, its continued approval is contingent upon verification of capmatinib's benefit in confirmatory trials. Capmatinib was approved by Health Canada on June 8, 2022.
Indication
用于治疗局部晚期或转移性MET外显子14跳跃（METEX 14）突变的非小细胞肺癌（NSCLC）患者。
Associated Conditions
- Metastatic Non-Small Cell Lung Cancer
- Unresectable, locally advanced Non-Small Cell Lung Carcinoma (NSCLC)
Research Report
Capmatinib (Tabrecta®): A Comprehensive Clinical and Pharmacological Monograph
Executive Summary
Capmatinib is a highly selective, orally bioavailable, adenosine triphosphate (ATP)-competitive inhibitor of the mesenchymal-epithelial transition (MET) receptor tyrosine kinase. Developed by Novartis, Capmatinib, marketed under the brand name Tabrecta®, represents a significant advancement in the field of precision oncology. Its mechanism of action is centered on the potent and specific inhibition of aberrant MET signaling, a key oncogenic driver in various malignancies. The drug is particularly effective against tumors harboring mutations that lead to MET exon 14 skipping (METex14), a specific genetic alteration that results in a constitutively active and stable MET protein.
Capmatinib was granted accelerated approval by the U.S. Food and Drug Administration (FDA) on May 6, 2020, becoming the first therapy specifically indicated for adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors harbor a METex14 mutation. This approval was based on compelling efficacy data from the pivotal GEOMETRY mono-1 Phase II clinical trial, which demonstrated substantial and durable tumor responses. In treatment-naïve patients, Capmatinib achieved an overall response rate of 68%, with a median duration of response of 12.6 months. In patients who had received prior therapy, the overall response rate was 41%, with a median duration of response of 9.7 months. These outcomes established a new standard of care for a patient population that previously lacked targeted therapeutic options.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/05/23 | Phase 2 | Recruiting | |||
2023/09/26 | Phase 2 | Not yet recruiting | Sun Yat-sen University | ||
2023/02/10 | Phase 2 | Recruiting | |||
2023/01/09 | N/A | Completed | |||
2022/12/08 | Phase 2 | Recruiting | |||
2022/10/05 | Phase 2 | Withdrawn | Timothy Burns, MD, PHD | ||
2022/08/04 | Phase 1 | Active, not recruiting | |||
2022/06/28 | Phase 1 | Terminated | Collin Blakely | ||
2022/02/17 | Phase 1 | Terminated | |||
2021/12/13 | N/A | Completed | Intergroupe Francophone de Cancerologie Thoracique |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| No FDA approvals found for this drug. | |||||
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| TABRECTA FILM-COATED TABLET 150mg | SIN16350P | TABLET, FILM COATED | 150mg | 10/22/2021 | |
| TABRECTA FILM-COATED TABLET 200mg | SIN16351P | TABLET, FILM COATED | 200mg | 10/22/2021 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
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 |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| No Health Canada approvals found for this drug. | |||||
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| No CIMA AEMPS (Spain) approvals found for this drug. | |||||
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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