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.

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

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]

See also

References

  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.