Drugs / Sitravatinib
last change Jun 2026 re-read 9 days ago

Sitravatinib

Small molecule targets AXL, DDR2, FLT3, KIT, MERTK, MET, RET, TYRO3 via inhibition

Developed for
non-small cell lung carcinoma · clear cell renal carcinoma · hepatocellular carcinoma · cancer · cancer of unknown primary site · biliary tract cancer · breast cancer · cervical cancer
+12 more · endometrial cancer · esophageal squamous cell carcinoma · gastroesophageal junction adenocarcinoma · liposarcoma · melanoma · oral cavity squamous cell carcinoma · small cell lung carcinoma · triple-negative breast carcinoma · ureter transitional cell carcinoma · urethra transitional cell carcinoma · urinary bladder cancer · uveal melanoma
Investigated by
Mirati Therapeutics Inc. · BeiGene · Fudan University · M.D. Anderson Cancer Center · Anhui Provincial Hospital · AstraZeneca
+20 more · Australia New Zealand Gynaecological Oncology Group · BeOne Medicines · Bristol-Myers Squibb · Cancer Research UK · Columbia University · Experimental Cancer Medicine Centres · First Affiliated Hospital Xi'an Jiaotong University · First Affiliated Hospital of Guangxi Medical University · Haider Mahdi · Henan Cancer Hospital · National Cancer Institute (NCI) · Peking University Cancer Hospital & Institute · Pfizer · Sarah Goldberg · Seoul National University Hospital · Spanish Melanoma Group · University Health Network, Toronto · University of Birmingham · Xiang Zhang · Zhejiang Cancer Hospital

Trials 34

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 01 trial
Phase 0 NCT03575598 Aug 2018 → Feb 2020 oral cavity squamous cell carcinoma University Health Network, Toronto Completed No outcome recorded
Phase 18 trials
Phase 1 NCT04935112 Jul → Aug 2021 — Mirati Therapeutics Inc. Completed No outcome recorded
Phase 1 NCT04887194 Apr 2021 → Dec 2022 — Mirati Therapeutics Inc. Completed No outcome recorded
Phase 1 NCT04800614 Mar → Jul 2021 — Mirati Therapeutics Inc. Completed No outcome recorded
Phase 1 NCT04772612 Mar 2021 → Jul 2022 — Mirati Therapeutics Inc. Completed No outcome recorded
Phase 1 NCT04518046 Aug 2020 → Jun 2023 clear cell renal carcinoma Mirati Therapeutics Inc. Completed No outcome recorded
Phase 1 NCT04472650 Jul → Nov 2020 neoplasm BeiGene Completed No outcome recorded
Phase 1 NCT03666143 Nov 2018 → Jan 2023 cancer BeiGene Completed No outcome recorded
Phase 1 NCT02219711 Aug 2014 → Apr 2022 cancer of unknown primary site Mirati Therapeutics Inc. Completed No outcome recorded
Phase 1/22 trials
Phase 1/2 NCT03941873 Feb 2019 → Mar 2023 gastroesophageal junction adenocarcinoma, hepatocellular carcinoma BeiGene Completed No outcome recorded
Phase 1/2 NCT03015740 Apr 2017 → Sep 2022 clear cell renal carcinoma M.D. Anderson Cancer Center Completed No outcome recorded
Phase 218 trials
Phase 2 NCT05614453 Jun 2023 cervical cancer Australia New Zealand Gynaecological Oncology Group Withdrawn No outcome recorded
Phase 2 NCT05461794 Oct 2022 → Feb 2024 esophageal squamous cell carcinoma BeiGene Terminated No outcome recorded Stop: Business
Phase 2 NCT05542342 Sep 2022 → Dec 2023 uveal melanoma Spanish Melanoma Group Completed No outcome recorded
Phase 2 NCT05419817 Sep 2022 → Jul 2025 endometrial cancer Haider Mahdi Withdrawn No outcome recorded Stop: Enrollment
Phase 2 NCT05407519 Jul 2022 → Jun 2026 hepatocellular carcinoma Anhui Provincial Hospital Unknown No outcome recorded
Phase 2 NCT04904302 May 2022 → Mar 2026 clear cell renal carcinoma M.D. Anderson Cancer Center Terminated No outcome recorded Stop: Business
Phase 2 NCT05228496 Mar 2022 → Jul 2023 small cell lung carcinoma Zhejiang Cancer Hospital Unknown No outcome recorded
Phase 2 NCT04925986 Feb 2022 → Jun 2023 non-small cell lung carcinoma Sarah Goldberg Terminated No outcome recorded Stop: Business
Phase 2 NCT05104801 Nov 2021 → Sep 2023 melanoma Peking University Cancer Hospital & Institute Unknown No outcome recorded
Phase 2 NCT04123704 Sep 2021 → Jan 2023 triple-negative breast carcinoma Xiang Zhang Terminated No outcome recorded
Phase 2/31 trial
Phase 2/3 NCT04887870 Jun 2021 → Apr 2025 cancer of unknown primary site Mirati Therapeutics Inc. Completed No outcome recorded
Phase 34 trials · 1 missed
Phase 3 NCT05564338 Jun 2023 → Apr 2027 hepatocellular carcinoma BeiGene Withdrawn No outcome recorded Stop: Business
Phase 3 NCT04921358 Jul 2021 → Dec 2023 non-small cell lung carcinoma BeiGene Terminated No outcome recorded
Phase 3 NCT04164199 Dec 2019 → May 2026 cancer BeOne Medicines Completed No outcome recorded
Phase 3 NCT03906071 Jul 2019 → Mar 2023 non-small cell lung carcinoma Mirati Therapeutics Inc. Terminated Missed primary
Comparator or background therapy1 trial
Phase 1 NCT05255276 Comparator Feb → May 2022 — Mirati Therapeutics Inc. Completed No outcome recorded

News releases announcing trial results or a regulatory action · 2

DateIssuerRelease
2021-04-11 BeOne Medicines Results BeiGene Presents Clinical Data on Sitravatinib in Combination with Tislelizumab at the AACR Annual Meeting 2021 beonemedicines.com ↗
The combination showed preliminary antitumor activity in patients with unresectable or metastatic melanoma refractory or resistant to PD-1/L1 inhibitors and platinum-resistant ovarian cancer in an ongoing Phase 1b clinical trial, with a generally well-tolerated safety profile.
2019-12-13 BeOne Medicines Results BeiGene Announces Clinical Data on Investigational Anti-PD-1 Antibody Tislelizumab in Combination with Sitravatinib at European Society for Medical Oncology Immuno-Oncology (ESMO I-O) Congress 2019 beonemedicines.com ↗

Evidence & citations 16 cited values

Every value below carries the sentence it was read from. 37 sources stand behind the page.

FieldValueCited text
Known as Sitravatinib ClinicalTrials.gov intervention name — accepted as the source's own label NCT03941873 ↗
32

NCT05407519 ↗

NCT04925986 ↗

NCT05564338 ↗

NCT03666143 ↗

NCT04727996 ↗

NCT04935112 ↗

NCT02954991 ↗

NCT03015740 ↗

NCT04518046 ↗

NCT04887870 ↗

Show 22 more sources

Known as MG-516 ChEMBL registry synonym — accepted as the source's own label CHEMBL3989926 ↗
Known as MG-91516 ChEMBL registry synonym — accepted as the source's own label CHEMBL3989926 ↗
Known as MGCD-516 L-MALATE ChEMBL registry synonym — accepted as the source's own label CHEMBL3989926 ↗
Known as MGCD-516 MALATE SALT ChEMBL registry synonym — accepted as the source's own label CHEMBL3989926 ↗
Known as MGCD516 “Sitravatinib (MGCD516) is an orally-available, potent small molecule inhibitor of a closely related spectrum of tyrosine kinases, which has shown antitumor activity in a...” NCT03575598 ↗
3

“efficacy (defined as achieving complete remission, partial remission, or stable disease within 6 weeks) of sitravatinib (MGCD516) when administered orally (PO) daily” NCT03015740 ↗

NCT02978859 ↗

NCT02219711 ↗

Known as Sitravatinib l-malate ChEMBL registry synonym — accepted as the source's own label CHEMBL3989926 ↗
Known as sitravatinib malate “A single-dose administration of sitravatinib malate 50 mg on Day 1.” NCT05255276 ↗
Action Inhibit “MGCD516 is a small molecule inhibitor of several closely related receptor tyrosine kinases.” NCT02219711 ↗
Modality Small molecule “MGCD516 is a small molecule inhibitor” NCT02219711 ↗
Route Oral “MGCD516 is orally administered to patients with advanced solid tumor malignancies” NCT02219711 ↗
Target AXL “MGCD516 is a receptor tyrosine kinase (RTK) inhibitor shown in preclinical models to inhibit a closely related spectrum of RTKs including MET, AXL, MER, and members of the...” NCT02219711 ↗
Target DDR2 “MGCD516 is a receptor tyrosine kinase (RTK) inhibitor shown in preclinical models to inhibit a closely related spectrum of RTKs including MET, AXL, MER, and members of the...” NCT02219711 ↗
Target MERTK “Sitravatinib (MGCD516), a spectrum-selective receptor tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MERTK)” PMID 35767205 ↗ Jun 2022
Target MET “MGCD516 is a receptor tyrosine kinase (RTK) inhibitor shown in preclinical models to inhibit a closely related spectrum of RTKs including MET, AXL, MER, and members of the...” NCT02219711 ↗
Target TYRO3 “Sitravatinib (MGCD516), a spectrum-selective receptor tyrosine kinase inhibitor targeting TAM (TYRO3, AXL, MERTK)” PMID 35767205 ↗ Jun 2022