Last reviewed · How we verify
Gavreto (PRALSETINIB)
Pralsetinib inhibits RET kinase and its oncogenic fusions/mutations, blocking downstream signaling and reducing tumor growth.
Gavreto (pralsetinib) is a small molecule kinase inhibitor developed by Blueprint Medicines and currently owned by Rigel Pharmaceuticals. It targets the proto-oncogene tyrosine-protein kinase receptor Ret, a protein involved in the growth and spread of cancer cells. Gavreto is FDA-approved for the treatment of medullary thyroid carcinoma and metastatic non-small cell lung cancer. It is a patented medication with no generic manufacturers available. Key safety considerations include potential liver damage and cardiovascular events.
At a glance
| Generic name | PRALSETINIB |
|---|---|
| Sponsor | Rigel Pharms |
| Drug class | Kinase Inhibitor [EPC] |
| Target | RET |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2020 |
Mechanism of action
Pralsetinib targets the RET kinase, which can be overactive due to fusions or mutations. By inhibiting RET, pralsetinib blocks the signals that lead to uncontrolled cell growth, thereby reducing tumor size and prolonging survival in animal models.
Approved indications
- Medullary thyroid carcinoma
- Metastatic non-small cell lung cancer
- Non-small cell lung cancer
Boxed warnings
- WARNING: SERIOUS INFECTIONS, INCLUDING OPPORTUNISTIC INFECTIONS GAVRETO may increase the risk for serious infections, including bacterial, fungal, viral and opportunistic infections, which can lead to hospitalization or death. Withhold, reduce the dose or permanently discontinue GAVRETO based on severity [see Dosage and Administration (2.3) , Warnings and Precautions (5.1) ] . WARNING: SERIOUS INFECTIONS, INCLUDING OPPORTUNISTIC INFECTIONS See full prescribing information for complete boxed warning. GAVRETO may increase the risk for serious infections, including bacterial, fungal, viral and opportunistic infections, which can lead to hospitalization or death. Withhold, reduce the dose or permanently discontinue GAVRETO based on severity. ( 2.3 , 5.1 )
Common side effects
- musculoskeletal pain
- constipation
- hypertension
- diarrhea
- fatigue
- edema
- pyrexia
- cough
Key clinical trials
- A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) (PHASE2)
- Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study (PHASE2)
- A Study of Pralsetinib Versus Standard of Care for First-Line Treatment of Advanced Non-Small Cell Lung Cancer (NSCLC) (PHASE3)
- Response to Neoadjuvant Treatment in Locally Advanced Thyroid Cancer
- A Real-world Study of Pralsetinib Combined With Leucogen in the Treatment of RET Fusion-positive NSCLC (NA)
- A Retrospective and Prospective Real-world Study of Molecular Typing in the Treatment of Advanced Thyroid Cancer (PHASE4)
- A Prospective Cohort Study of Pralsetinib or Anlotinib in the Treatment of Locally Advanced and/or Metastatic Medullary Thyroid Carcinoma With RET Gene Mutations
- Genotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study (PHASE4)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Gavreto CI brief — competitive landscape report
- Gavreto updates RSS · CI watch RSS
- Rigel Pharms portfolio CI