| Stereochemistry | ABSOLUTE |
| Molecular Formula | C18H39N7O3 |
| Molecular Weight | 401.5474 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](N)CCNCCCCNC(=O)OCC(=O)NCCCCCCNC(N)=N
InChI
InChIKey=PZDPVSFZTKORSP-OAHLLOKOSA-N
InChI=1S/C18H39N7O3/c1-15(19)8-13-22-9-6-7-12-25-18(27)28-14-16(26)23-10-4-2-3-5-11-24-17(20)21/h15,22H,2-14,19H2,1H3,(H,23,26)(H,25,27)(H4,20,21,24)/t15-/m1/s1
Anisperimus [LF 150195] is a deoxyspergualin analogue under development by Fournier Pharma (formerly Groupe Fournier) for the potential treatment of autoimmune disorders and transplant rejection. Anisperimus is a more potent, and less toxic analogue of 15-deoxyspergualin, an antibiotic used as an immunosuppressive agent to prevent rejection of organ transplants. Anisperimus enhances activation-induced T-cell death by facilitating caspase-8 and caspase-10 activation at the DISC level. Phase I clinical studies were being conducted by Fournier in France for Transplant rejection and Phase II clinical studies for Autoimmune disorders in Europe. However development of anisperimus has been discontinued.
Originator
Approval Year
PubMed
Sample Use Guides
Monkeys: Recipients received Anisperimus monotherapy at doses of 0.065 mg/kg per day (group 2, n=4), 0.13 mg/kg per day (group 3, n=4), or 0.2 mg/kg per day (group 4, n=4), administered subcutaneously, on postoperative days 0 to 14.
Route of Administration:
Other
Hoechst 33342 staining of the nuclear chromatin indicated thatexposure of Jurkat cells to Anisperimus [LF 150195] sensitized these cells to apoptosis triggered by various concentrations of CH-11 mAb and at various time points. Analysis of the dose-dependent effects of LF 15-0195 indicated that 0.1 uM was an optimal concentration for further studies. Higher concentra-tions such as 1uM and 10uM did not demonstrate significantly higher sensitization to 5 ng/mL CH11 anti-CD95 mAb. The 0.1uM concentration is about 10-fold lower than plasma levels measured in rats and monkeys receiving anintravenous injection of the studied compound.
ACTIVE MOIETY
