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Sitravatinib

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Sitravatinib
Clinical data
ATC code
Identifiers
  • 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
ChemSpider
UNII
KEGG
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC33H29F2N5O4S
Molar mass629.68 g·mol−1
3D model (JSmol)
  • COCCNCc1ccc(nc1)c2cc3c(s2)c(ccn3)Oc4ccc(cc4F)NC(=O)C5(CC5)C(=O)Nc6ccc(cc6)F
  • 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 multipletyrosine kinases.[1]

Sitravatinib is being developed byMirati Therapeutics.[2]

Ongoingphase II trials include a trial for liposarcoma,[3] a combination trial fornon-small cell lung cancer,[4] and a combination trial withnivolumab forrenal 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 tocheckpoint inhibitor therapy, and certain patients who are naïve to checkpoint inhibitor therapy.[6]

References

[edit]
  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 numberNCT02978859 for "MGCD516 in Advanced Liposarcoma and Other Soft Tissue Sarcomas" atClinicalTrials.gov
  4. ^Clinical trial numberNCT02954991 for "Phase 2 Study of Glesatinib, Sitravatinib or Mocetinostat in Combination With Nivolumab in Non-Small Cell Lung Cancer" atClinicalTrials.gov
  5. ^Clinical trial numberNCT03015740 for "MGCD516 Combined With Nivolumab in Renal Cell Cancer (RCC)" atClinicalTrials.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.
CImonoclonal antibodies ("-mab")
Receptor tyrosine kinase
Others for solid tumors
Leukemia/lymphoma
Other
Tyrosine kinase inhibitors ("-nib")
Receptor tyrosine kinase
Non-receptor
Other
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