Forodesine

Forodesine
Clinical data
Trade namesMundesine and Fodosine
Routes of
administration		oral
Identifiers
  • 7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-1,5-dihydropyrrolo[2,3-e]pyrimidin-4-one
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC11H14N4O4
Molar mass266.257 g·mol−1
3D model (JSmol)
  • C1=C(C2=C(N1)C(=O)NC=N2)[C@H]3[C@@H]([C@@H]([C@H](N3)CO)O)O
  • InChI=1S/C11H14N4O4/c16-2-5-9(17)10(18)7(15-5)4-1-12-8-6(4)13-3-14-11(8)19/h1,3,5,7,9-10,12,15-18H,2H2,(H,13,14,19)/t5-,7+,9-,10+/m1/s1
  • Key:IWKXDMQDITUYRK-KUBHLMPHBW

  • InChI=1/C11H14N4O4/c16-2-5-9(17)10(18)7(15-5)4-1-12-8-6(4)13-3-14-11(8)19/h1,3,5,7,9-10,12,15-18H,2H2,(H,13,14,19)/t5-,7+,9-,10+/m1/s1

Forodesine (INN; also known as Immucillin H; trade names Mundesine and Fodosine) is a transition-state analog inhibitor of purine nucleoside phosphorylase[1] studied for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and for treatment of B-cell acute lymphocytic leukemia (B-ALL).

Forodesine was originally discovered by Vern Schramm's laboratory at the Albert Einstein College of Medicine in New York and Industrial Research Limited in New Zealand.[citation needed]

Forodesine is being developed by BioCryst Pharmaceuticals. As of 2008, it is currently in phase II clinical trials.[2][needs update].

In 2006, BioCryst entered into a licensing agreement with Mundipharma International Holdings Limited to develop and commercialize forodesine in markets across Europe, Asia, and Australasia for use in oncology.[3]

In April 2017, forodesine was approved in Japan for the treatment of relapsed/refractory peripheral T-cell lymphoma.[4][5]

  1. ^ Kicska GA, Long L, Hörig H, Fairchild C, Tyler PC, Furneaux RH, et al. (April 2001). "Immucillin H, a powerful transition-state analog inhibitor of purine nucleoside phosphorylase, selectively inhibits human T lymphocytes". Proceedings of the National Academy of Sciences of the United States of America. 98 (8): 4593–4598. Bibcode:2001PNAS...98.4593K. doi:10.1073/pnas.071050798. PMC 31879. PMID 11287638.
  2. ^ "Complete list of clinical trials for forodesine (BCX-1777) (ClinicalTrials.gov)". Retrieved 2008-07-22.
  3. ^ "Biocryst Initiates Pivotal Fodosine Phase IIb Clinical Trial In Patients With Relapsed/Refractory T-Lymphoblastic Leukemia/Lymphoma" (Press release). January 16, 2007.
  4. ^ "BioCryst Announces Mundipharma Receives Approval for Mundesine in Japan" (Press release). April 3, 2017.
  5. ^ Makita S, Maeshima AM, Maruyama D, Izutsu K, Tobinai K (2018). "Forodesine in the treatment of relapsed/refractory peripheral T-cell lymphoma: an evidence-based review". OncoTargets and Therapy. 11: 2287–2293. doi:10.2147/OTT.S140756. PMC 5916385. PMID 29719411.