Chemistry:Sitravatinib

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Short description: Chemical compound
Sitravatinib
Sitravatinib.svg
Clinical data
ATC code
Identifiers
CAS Number
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC33H29F2N5O4S
Molar mass629.68 g·mol−1
3D model (JSmol)

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

  1. "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. doi:10.1002/cac2.12040. PMID 32525624. 
  2. "Sitravatinib | Mirati Therapeutics, Inc". http://www.mirati.com/go/mgcd516/. 
  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. https://clinicaltrials.gov/ct2/show/NCT03906071.