Drugs / Sitravatinib
last change Jun 2026 re-read 2 minutes 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 · a red edge is where a trial was stopped

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
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
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
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
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
Phase 3 NCT05564338 Jun 2023 → Apr 2027 hepatocellular carcinoma BeiGene Withdrawn No outcome recorded
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. Completed No outcome recorded
Also used as a comparator or background therapy in 1 trial
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 1 NCT05255276 Comparator Feb → May 2022 Mirati Therapeutics Inc. Completed No outcome recorded

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 NCT04164199
32

NCT05614453

NCT04518046

NCT04935112

NCT04472650

NCT03666143

NCT03575598

NCT05228496

NCT02664935

NCT05419817

NCT04772612

NCT02954991

NCT05542342

NCT03906071

NCT04123704

NCT05255276

NCT04904302

NCT05176925

NCT04734262

NCT04887870

NCT04921358

NCT03015740

NCT03941873

NCT03606174

NCT05461794

NCT04800614

NCT05407519

NCT04727996

NCT04887194

NCT05564338

NCT05104801

NCT04925986

NCT03680521

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

NCT02219711

NCT02978859

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