Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H27N5O6 |
Molecular Weight | 433.4583 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCOC(=O)N[C@@H](CNC(=O)C[C@H]1CC(=NO1)C2=CC=C(C=C2)C(N)=N)C(O)=O
InChI
InChIKey=SRRJCHGGTPFZSS-ZBFHGGJFSA-N
InChI=1S/C20H27N5O6/c1-2-3-8-30-20(29)24-16(19(27)28)11-23-17(26)10-14-9-15(25-31-14)12-4-6-13(7-5-12)18(21)22/h4-7,14,16H,2-3,8-11H2,1H3,(H3,21,22)(H,23,26)(H,24,29)(H,27,28)/t14-,16+/m1/s1
Roxifiban (also known as DMP754), a potent antiplatelet agent in inhibiting platelet aggregation, and has a high specificity and affinity for human platelet glycoprotein IIb/IIIa complex (GPIIb/IIIa) receptors. Roxifiban participated in clinical trials phase III for the treatment of peripheral arterial disorders. This drug was also well tolerated in patients with chronic stable angina pectoris and was studied in the treatment of heparin-induced thrombocytopenia, and thrombosis. However, the development of this drug appears to have been discontinued.
Approval Year
PubMed
Title | Date | PubMed |
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Oral antiplatelet efficacy of the platelet GPIIb/IIIa antagonist, DMP754 in non-human primates. | 1998 Mar 1 |
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Comparative efficacy between the glycoprotein IIb/IIIa antagonists roxifiban and orbofiban in inhibiting platelet responses in flow models of thrombosis. | 2002 Apr |
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The use of roxifiban (DMP754), a novel oral platelet glycoprotein IIb/IIIa receptor inhibitor, in patients with stable coronary artery disease. | 2003 |
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[Long-lasting thrombocytopenia induced by glycoprotein IIb/IIIa inhibitor]. | 2017 Nov |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/14727937
Ninety-eight patients were randomized to receive either a placebo or 1 of 8 oral dosages of roxifiban. Twenty-two patients were enrolled in multiple-dose regimens, bringing the total study population to 120. The oral dosages were 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, or 2.5 mg/day for up to 30 days.
Route of Administration:
Oral
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170902-52-0
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177231
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R96EWZ6KUZ
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admin on Sat Dec 16 19:51:25 GMT 2023 , Edited by admin on Sat Dec 16 19:51:25 GMT 2023
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ACTIVE MOIETY
PRODRUG (METABOLITE ACTIVE)