Chemistry:Ciforadenant
Ciforadenant (INN, USAN; developmental code names CPI-444 and V-81444) is an adenosine A2A receptor antagonist which is under development for the treatment of renal cell carcinoma and non-small cell lung cancer.[1][2][3][4][5][6] It is or was also under development for the treatment of attention-deficit hyperactivity disorder (ADHD), cancer, multiple myeloma, Parkinson's disease, and solid tumors, but no recent development has been reported for these indications.[1][2][4] The drug is taken orally.[1]
It shows high affinity for the adenosine A2A receptor (Ki = 3.54 nM) and high selectivity for this receptor over the other adenosine receptors (54- to 693-fold).[6] The elimination half-life of ciforadenant is 3 hours with a single dose and 10.2 to 10.6 hours with multiple repeated doses in humans.[3]
Ciforadenant was originated by Vernalis and is under development by Corvus Pharmaceuticals.[1][2] As of January 2026, it is in phase 2 clinical trials for renal cell carcinoma and phase 1/2 trials for non-small cell lung cancer, whereas there has been no recent development for other uses.[1][2]
See also
- List of investigational attention deficit hyperactivity disorder drugs
- List of investigational Parkinson's disease drugs
References
- ↑ 1.0 1.1 1.2 1.3 1.4 "Corvus Pharmaceuticals". 28 January 2026. https://adisinsight.springer.com/drugs/800034823.
- ↑ 2.0 2.1 2.2 2.3 "Delving into the Latest Updates on Ciforadenant with Synapse". 12 May 2026. https://synapse.patsnap.com/drug/666bfafeca114b83a91404fe304c43f8.
- ↑ 3.0 3.1 "CIFORADENANT". https://drugs.ncats.io/substance/8KFO2187CP.
- ↑ 4.0 4.1 "Adenosine A2A receptor antagonists in Parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued". CNS Drugs 28 (5): 455–474. May 2014. doi:10.1007/s40263-014-0161-7. PMID 24687255.
- ↑ "Adenosine 2A Receptor Blockade as an Immunotherapy for Treatment-Refractory Renal Cell Cancer". Cancer Discovery 10 (1): 40–53. January 2020. doi:10.1158/2159-8290.CD-19-0980. PMID 31732494.
- ↑ 6.0 6.1 "Tumor Immunotherapy Using A2A Adenosine Receptor Antagonists". Pharmaceuticals (Basel) 13 (9): 237. September 2020. doi:10.3390/ph13090237. PMID 32911819. "CPI-444 (ciforadenant, previously known as V-81444) is an orally available A2AAR antagonist created by Vernalis [64]. [...] It showed a binding affinity of 3.54 nM for A2AAR, with 54-, 431-, and 693-fold selectivity against A1AR, A2BAR, and A3AR, respectively (Table 1) [19]. In functional assays, CPI-444 showed an IC50 of 70 nM in the G protein-mediated cAMP assay [19]".
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