Sitravatinib Explained

Iupac Name:	N-(3-Fluoro-4-phenyl)-N′-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
Cas Number:	1123837-84-2
Unii:	CWG62Q1VTB
Atc Prefix:	L01
Atc Suffix:	EX26
Chemspiderid:	52083477
Kegg:	D11140
C:	33
H:	29
F:	2
N:	5
O:	4
S:	1
Smiles:	COCCNCc1ccc(nc1)c2cc3c(s2)c(ccn3)Oc4ccc(cc4F)NC(=O)C5(CC5)C(=O)Nc6ccc(cc6)F
Stdinchi:	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)
Stdinchikey:	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, a combination trial for non-small cell lung cancer, and a combination trial with nivolumab for renal cell carcinoma. 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.^[3]

Notes and References

Yang Y, Ji N, Cai CY, Wang JQ, Lei ZN, Teng QX, Wu ZX, Cui Q, Pan Y, Chen ZS . Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor . Cancer Communications . 40 . 7 . 285–300 . July 2020 . 32525624 . 7365458 . 10.1002/cac2.12040 .
Web site: Sitravatinib | Mirati Therapeutics, Inc.
Web site: 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.