Drugs / Pralsetinib
last change Jun 2026 re-read 2 minutes ago

Pralsetinib

Small molecule targets RET via inhibition

Developed for
non-small cell lung carcinoma · medullary thyroid gland carcinoma · RET fusion positive cancer · breast cancer · cancer · cancer of unknown primary site · colorectal cancer · digestive system cancer
+4 more · lung carcinoma · thyroid gland carcinoma · thyroid gland papillary carcinoma · thyroid tumor
Investigated by
Hoffmann-La Roche · Fudan University · Genentech, Inc. · Sun Yat-sen University · Blueprint Medicines Corporation · Changhai Hospital
+26 more · Dalian Friendship Hospital Affiliated to Dalian Medical University · Fondazione per la Medicina Personalizzata · Fujian Cancer Hospital · Fujian Medical University · Henan Cancer Hospital · Hunan Province Tumor Hospital · Hunan Provincial People's Hospital · Jiangsu Cancer Institute & Hospital · Liaoning Cancer Hospital & Institute · Peking Union Medical College Hospital · Rigel Pharmaceuticals · 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 · Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University · The Affiliated Hospital of Inner Mongolia Medical University · The First Affiliated Hospital of Anhui University of Chinese Medicine · 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 · West China Hospital · Zhejiang Cancer Hospital

Regulatory milestones approvals, filings & regulatory actions · 4 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Withdrawn EU (EMA) Gavreto 2024-10-24 europa.eu
Label expansion US (FDA) GAVRETO 2023-08-09 fda.gov
Approved · conditional EU (EMA) Gavreto 2021-11-18 europa.eu
Approved US (FDA) GAVRETO 2020-09-04 fda.gov

Trials 15 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 1/21 trial
Phase 1/2 NCT03037385 Mar 2017 → Mar 2024 bronchogenic carcinoma, colonic neoplasm, colorectal cancer, head and neck neoplasm +4 Hoffmann-La Roche Completed No outcome recorded
Phase 27 trials
Phase 2 NCT06563999 Nov 2024 → Nov 2027 expected lung carcinoma Sun Yat-sen University Recruiting No outcome recorded
Phase 2 NCT06482086 Jun 2021 → Dec 2024 overdue thyroid gland carcinoma West China Hospital Recruiting No outcome recorded
Phase 2 NCT04589845 Jan 2021 → Sep 2032 expected cancer Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 2 NCT04632992 Jan 2021 → Dec 2023 cancer of unknown primary site Genentech, Inc. Completed No outcome recorded
Phase 2 NCT04302025 Nov 2020 → Nov 2026 expected non-small cell lung carcinoma Genentech, Inc. 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 NCT04322890 Apr 2020 → Dec 2026 expected non-small cell lung carcinoma Hunan Province Tumor Hospital Recruiting No outcome recorded
Phase 32 trials
Phase 3 NCT04760288 Nov 2023 → Oct 2027 medullary thyroid gland carcinoma Hoffmann-La Roche Withdrawn No outcome recorded
Phase 3 NCT04222972 Jul 2020 → Jan 2025 RET fusion positive cancer, adenocarcinoma, bronchogenic carcinoma, germ cell tumor +3 Hoffmann-La Roche Terminated No outcome recorded
Phase 43 trials
Phase 4 NCT07704658 Jun 2026 → Jul 2027 expected non-small cell lung carcinoma, thyroid cancer Rigel Pharmaceuticals Recruiting No outcome recorded
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 applicable1 trial
NCT07418879 Feb 2026 → Dec 2027 expected RET fusion positive cancer, non-small cell lung carcinoma Fudan University Not yet recruiting No outcome recorded
Phase not stated1 trial
NCT04204928 medullary thyroid gland carcinoma, non-small cell lung carcinoma Blueprint Medicines Corporation Approved for marketing No outcome recorded

Press releases naming this drug 4 releases

DateIssuerRelease
2021-11-19 Roche Global Development European Commission approves Roche’s Gavreto (pralsetinib) for the treatment of adults with RET fusion-positive advanced non-small cell lung cancer roche.com
2021-09-17 Roche Global Development Roche receives positive CHMP opinion for Gavreto® (pralsetinib) for the treatment of adults with RET fusion-positive advanced non-small cell lung cancer roche.com
2020-12-02 Roche Global Development Roche announces FDA approval of Gavreto (pralsetinib) for people with advanced or metastatic RET-mutant and RET fusion-positive thyroid cancers roche.com
2020-09-07 Roche Global Development Roche announces FDA approval of Gavreto (pralsetinib) for the treatment of adults with metastatic RET fusion-positive non-small cell lung cancer roche.com

Evidence & citations 13 cited values

Every value below carries the sentence it was read from. 16 sources stand behind the page.

FieldValueCited text
Known as Pralsetinib Pralsetinib etc.” NCT04322890
14

NCT04589845

NCT03037385

NCT04222972

NCT04760288

NCT04204928

NCT06563999

NCT04591431

NCT07704658

NCT06195228

NCT07010393

NCT07418879

NCT04632992

NCT04302025

NCT06482086

Known as BLU-123244 ChEMBL registry synonym — accepted as the source's own label CHEMBL4582651
Known as BLU-667 “pralsetinib (BLU-667)” NCT04204928
Known as CIS-PRALSETINIB ChEMBL registry synonym — accepted as the source's own label CHEMBL4582651
Known as CT-BLU667BLU-667BLU667 ChEMBL registry synonym — accepted as the source's own label CHEMBL4582651
Known as GAVRETO ChEMBL registry synonym — accepted as the source's own label CHEMBL4582651
Known as Pralsetinib, cis- ChEMBL registry synonym — accepted as the source's own label CHEMBL4582651
Known as RG-6396 ChEMBL registry synonym — accepted as the source's own label CHEMBL4582651
Known as X-581238 ChEMBL registry synonym — accepted as the source's own label CHEMBL4582651
Action Inhibit “pralsetinib (BLU-667) is a potent and selective inhibitor of the RET mutations, fusions, and predicted resistant mutants” NCT03037385
Modality Small molecule CHEMBL4582651
Route Oral “pralsetinib (BLU-667) administered orally” NCT03037385
Target RET “inhibitor of the RET mutations, fusions, and predicted resistant mutants” NCT03037385