Gusperimus

Gusperimus
Skeletal formula of a gusperimus minor tautomer
Skeletal formula of a gusperimus minor tautomer
Names
Other names
N-[2-[4-(3-Aminopropylamino)butylamino]-1-hydroxy-2-oxoethyl]-7-(diaminomethylideneamino)heptanamide[1]
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
MeSH gusperimus
UNII
  • InChI=1S/C17H37N7O3/c18-9-7-11-21-10-5-6-12-22-15(26)16(27)24-14(25)8-3-1-2-4-13-23-17(19)20/h16,21,27H,1-13,18H2,(H,22,26)(H,24,25)(H4,19,20,23) checkY
    Key: IDINUJSAMVOPCM-UHFFFAOYSA-N checkY
  • N=C(N)NCCCCCCC(=O)NC(O)C(=O)NCCCCNCCCN
Properties
C17H37N7O3
Molar mass 387.529 g·mol−1
log P −0.933
Acidity (pKa) 11.588
Basicity (pKb) 2.409
Pharmacology
L04AA19 (WHO)
  • Intravenous
  • Subcutaneous
Pharmacokinetics:
100%
Legal status
  • In general: ℞ (Prescription only)
Related compounds
Related compounds
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Gusperimus is an immunosuppressive drug. It is a derivative of the naturally occurring HSP70 inhibitor spergualin, and inhibits the interleukin-2-stimulated maturation of T cells to the S and G2/M phases and the polarization of the T cells into IFN-gamma-secreting Th1 effector T cells, resulting in the inhibition of growth of activated naive CD4 T cells.

Gusperimus was developed by Bristol-Myers Squibb. Currently, it is manufactured and sponsored for use as an orphan drug and for clinical studies by the Japanese company Euro Nippon Kayaku. The patent claim (see quotation) is that Gusperimus may be useful for a variety of hyperreactive inflammatory diseases such as autoimmune diseases. The drug is available in vials containing 100 mg each.

There is little information about the pharmacokinetic properties of gusperimus.

  1. ^ "gusperimus - Compound Summary". PubChem Compound. USA: National Center for Biotechnology Information. 27 March 2005. Identification. Retrieved 4 July 2012.

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