Rabacfosadine succinate Chemical Properties

InChI

InChI=1/C21H35N8O6P.C4H6O4/c1-5-34-19(30)13(3)27-36(32,28-14(4)20(31)35-6-2)12-33-10-9-29-11-23-16-17(24-15-7-8-15)25-21(22)26-18(16)29;5-3(6)1-2-4(7)8/h11,13-15H,5-10,12H2,1-4H3,(H2,27,28,32)(H3,22,24,25,26);1-2H2,(H,5,6)(H,7,8)/t13-,14-;/s3

InChIKey

XLBDQSJWTNREFA-FGVWXQOBNA-N

SMILES

C(C(=O)O)CC(=O)O.C(N1C=NC2=C(N=C(N)N=C12)NC1CC1)COCP(=O)(N[C@@H](C)C(=O)OCC)N[C@@H](C)C(=O)OCC |&1:29,37,r|

Rabacfosadine succinate Usage And Synthesis

Description

Rabacfosadine succinate, also known as VDC-1101 or GS-9219, is a double prodrug of the nucleotide analogue 9-(2-phosphonylmethoxyethl)guanine (PMEG). It is a novel chemotherapy drug approved for the treatment of lymphoma in dogs. Rabacfosadine administered every 3 weeks is usually well tolerated and has shown significant anti-tumour activity in dogs with previously untreated medium and large cell lymphoma.

Uses

Rabacfosadine succinate is used as the acyclic nucleoside phosphonate PMEG double prodrug.

Mechanism of action

Rabacfosadine succinate targets lymphocytes and acts as an anti-tumour agent by inhibiting DNA synthesis through the inhibition of DNA polymerase.

Side effects

The most common adverse reaction to Rabacfosadine succinate is gastrointestinal (anorexia/diarrhoea), which is generally resolved by supportive therapy and/or dose adjustment. Three dogs developed VCOG-CTCAE grade 5 delayed pulmonary fibrosis.