Linrodostat (development code BMS-986205) is an experimental drug being studied for its immunomodulating and antineoplastic activities.[1]

Linrodostat
Clinical data
Other namesBMS-986205; ONO 7701
Routes of
administration
Oral
Legal status
Legal status
  • Investigational
Identifiers
  • (2R)-N-(4-Chlorophenyl)-2-[(1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide
CAS Number
DrugBank
ChemSpider
UNII
Chemical and physical data
FormulaC24H24ClFN2O
Molar mass410.92 g·mol−1
3D model (JSmol)
  • FC1=CC=2C(=CC=NC2C=C1)[C@@H]3CC[C@]([C@H](C(NC4=CC=C(Cl)C=C4)=O)C)(CC3)[H]
  • InChI=1S/C24H24ClFN2O/c1-15(24(29)28-20-9-6-18(25)7-10-20)16-2-4-17(5-3-16)21-12-13-27-23-11-8-19(26)14-22(21)23/h6-17H,2-5H2,1H3,(H,28,29)/t15-,16-,17+/m1/s1
  • Key:KRTIYQIPSAGSBP-ZACQAIPSSA-N

Linrodostat is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1).[2][3]

Linrodostat has entered clinical trials for a variety of cancer types including bladder cancer, head and neck cancer, endometrial cancer, gastric cancer, malignant melanoma, liver cancer, non-small cell lung cancer, and solid tumors.[4]

References

edit
  1. ^ "Linrodostat". NCI Drug Dictionary. National Cancer Institute.
  2. ^ Balog A, Lin TA, Maley D, Gullo-Brown J, Kandoussi EH, Zeng J, Hunt JT (March 2021). "Preclinical Characterization of Linrodostat Mesylate, a Novel, Potent, and Selective Oral Indoleamine 2,3-Dioxygenase 1 Inhibitor". Molecular Cancer Therapeutics. 20 (3): 467–476. doi:10.1158/1535-7163.MCT-20-0251. PMID 33298590. S2CID 228087398.
  3. ^ "IDO Inhibitor Development Shows Fresh Signs of Life Across Tumor Types". onclive.com. October 31, 2019.
  4. ^ "Linrodostat". Adis Insight. Springer Nature Switzerland AG.
edit
  • Fraunhoffer KJ, Delmonte AJ, Beutner GL, Bultman MS, Camacho K, Cohen B, et al. (2019). "Rapid Development of a Commercial Process for Linrodostat, an Indoleamine 2,3-Dioxygenase (IDO) Inhibitor". Organic Process Research & Development. 23 (11): 2482–2498. doi:10.1021/acs.oprd.9b00359. S2CID 208690975.