Ciforadenant

Ciforadenant
Clinical data
Other namesCPI-444; CPI444; V-81444; V81444; BIIB34
Routes of
administration		Oral[1]
Drug classAdenosine A2A receptor antagonist
ATC code
  • None
Pharmacokinetic data
Elimination half-lifeSingle: 3 hours[2]
Multiple: 10.2–10.6 hours[2]
Identifiers
  • 7-(5-methylfuran-2-yl)-3-[[6-[[(3S)-oxolan-3-yl]oxymethyl]-2-pyridinyl]methyl]triazolo[4,5-d]pyrimidin-5-amine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC20H21N7O3
Molar mass407.434 g·mol−1
3D model (JSmol)
  • CC1=CC=C(O1)C2=C3C(=NC(=N2)N)N(N=N3)CC4=NC(=CC=C4)CO[C@H]5CCOC5
  • InChI=1S/C20H21N7O3/c1-12-5-6-16(30-12)17-18-19(24-20(21)23-17)27(26-25-18)9-13-3-2-4-14(22-13)10-29-15-7-8-28-11-15/h2-6,15H,7-11H2,1H3,(H2,21,23,24)/t15-/m0/s1
  • Key:KURQKNMKCGYWRJ-HNNXBMFYSA-N

Ciforadenant (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; 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][3][2][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][3][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.[2]

Ciforadenant was originated by Vernalis and is under development by Corvus Pharmaceuticals.[1][3] 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][3]

See also

References

  1. 1 2 3 4 5 6 "Corvus Pharmaceuticals". AdisInsight. 28 January 2026. Retrieved 27 May 2026.
  2. 1 2 3 4 "CIFORADENANT". Inxight Drugs. Retrieved 27 May 2026.
  3. 1 2 3 4 "Delving into the Latest Updates on Ciforadenant with Synapse". Synapse. 12 May 2026. Retrieved 27 May 2026.
  4. 1 2 Pinna A (May 2014). "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. doi:10.1007/s40263-014-0161-7. PMID 24687255.
  5. ↑ Fong L, Hotson A, Powderly JD, Sznol M, Heist RS, Choueiri TK, et al. (January 2020). "Adenosine 2A Receptor Blockade as an Immunotherapy for Treatment-Refractory Renal Cell Cancer". Cancer Discovery. 10 (1): 40–53. doi:10.1158/2159-8290.CD-19-0980. PMC 6954326. PMID 31732494.
  6. 1 2 Zhang J, Yan W, Duan W, Wüthrich K, Cheng J (September 2020). "Tumor Immunotherapy Using A2A Adenosine Receptor Antagonists". Pharmaceuticals. 13 (9). Basel: 237. doi:10.3390/ph13090237. PMC 7558881. 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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