Sitravatinib

Sitravatinib
Clinical data
ATC code	L01EX26 (WHO) ;
Identifiers
	IUPAC name N-(3-Fluoro-4-{[2-(5-{[(2-methoxyethyl)amino]methyl}-2-pyridinyl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)-N′-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide;
CAS Number	1123837-84-2;
ChemSpider	52083477;
UNII	CWG62Q1VTB;
KEGG	D11140;
CompTox Dashboard (EPA)	DTXSID801100124 ;
Chemical and physical data
Formula	C33H29F2N5O4S
Molar mass	629.68 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COCCNCc1ccc(nc1)c2cc3c(s2)c(ccn3)Oc4ccc(cc4F)NC(=O)C5(CC5)C(=O)Nc6ccc(cc6)F;
	InChI InChI=1S/C33H29F2N5O4S/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42); Key:WLAVZAAODLTUSW-UHFFFAOYSA-N;

Sitravatinib (MGCD516) is an experimental drug for the treatment of cancer. It is a small molecule inhibitor of multiple tyrosine kinases.^[1]

Sitravatinib is being developed by Mirati Therapeutics.^[2]

Ongoing phase II trials include a trial for liposarcoma,^[3] a combination trial for non-small cell lung cancer,^[4] and a combination trial with nivolumab for renal cell carcinoma.^[5] Sitravatinib is being evaluated in ongoing trials in patients with advanced non-small cell lung cancer, including in a combination trial with nivolumab in those who are resistant to checkpoint inhibitor therapy, and certain patients who are naïve to checkpoint inhibitor therapy.^[6]

References

^ Yang Y, Ji N, Cai CY, Wang JQ, Lei ZN, Teng QX, Wu ZX, Cui Q, Pan Y, Chen ZS (July 2020). "Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor". Cancer Communications. 40 (7): 285–300. doi:10.1002/cac2.12040. PMC 7365458. PMID 32525624.
^ "Sitravatinib | Mirati Therapeutics, Inc".
^ Clinical trial number NCT02978859 for "MGCD516 in Advanced Liposarcoma and Other Soft Tissue Sarcomas" at ClinicalTrials.gov
^ Clinical trial number NCT02954991 for "Phase 2 Study of Glesatinib, Sitravatinib or Mocetinostat in Combination With Nivolumab in Non-Small Cell Lung Cancer" at ClinicalTrials.gov
^ Clinical trial number NCT03015740 for "MGCD516 Combined With Nivolumab in Renal Cell Cancer (RCC)" at ClinicalTrials.gov
^ "A Randomized Phase 3 Study of Sitravatinib in Combination with Nivolumab Versus Docetaxel in Patients with Advanced Non-Squamous Non-Small Cell Lung Cancer with Disease Progression on or After Platinum-Based Chemotherapy and Checkpoint Inhibitor Therapy SAPPHIRE". 28 February 2022.

[pmid32525624-1] Yang Y, Ji N, Cai CY, Wang JQ, Lei ZN, Teng QX, Wu ZX, Cui Q, Pan Y, Chen ZS (July 2020). "Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor". Cancer Communications. 40 (7): 285–300. doi:10.1002/cac2.12040. PMC 7365458. PMID 32525624.

[2] "Sitravatinib | Mirati Therapeutics, Inc".

[3] Clinical trial number NCT02978859 for "MGCD516 in Advanced Liposarcoma and Other Soft Tissue Sarcomas" at ClinicalTrials.gov

[4] Clinical trial number NCT02954991 for "Phase 2 Study of Glesatinib, Sitravatinib or Mocetinostat in Combination With Nivolumab in Non-Small Cell Lung Cancer" at ClinicalTrials.gov

[5] Clinical trial number NCT03015740 for "MGCD516 Combined With Nivolumab in Renal Cell Cancer (RCC)" at ClinicalTrials.gov

[6] "A Randomized Phase 3 Study of Sitravatinib in Combination with Nivolumab Versus Docetaxel in Patients with Advanced Non-Squamous Non-Small Cell Lung Cancer with Disease Progression on or After Platinum-Based Chemotherapy and Checkpoint Inhibitor Therapy SAPPHIRE". 28 February 2022.

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