Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C28H39N6O8P |
| Molecular Weight | 618.6184 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCOC(=O)N1CCN(CC1)C(=O)[C@H](CP(O)(O)=O)NC(=O)C2=NC(=NC(=C2)N3CC[C@@H](C3)OC)C4=CC=CC=C4
InChI
InChIKey=FYXHWMQPCJOJCH-GMAHTHKFSA-N
InChI=1S/C28H39N6O8P/c1-3-4-16-42-28(37)33-14-12-32(13-15-33)27(36)23(19-43(38,39)40)30-26(35)22-17-24(34-11-10-21(18-34)41-2)31-25(29-22)20-8-6-5-7-9-20/h5-9,17,21,23H,3-4,10-16,18-19H2,1-2H3,(H,30,35)(H2,38,39,40)/t21-,23-/m0/s1
| Molecular Formula | C28H39N6O8P |
| Molecular Weight | 618.6184 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
ACT-281959 (molecular weight 850.9 g/mol), the di-ester prodrug of
ACT-246475 (molecular weight 618.6 g/mol), was developed to improve absorption after oral dosing and is rapidly converted by esterases in vivo to ACT-246475 in two-steps via the formation of ACT-409100 (molecular weight 734.7 g/mol), the mono-ester prodrug. ACT-281959 is a novel potent and selective P2Y12 receptor antagonist with a wider therapeutic window. ACT-281959 showed antithrombotic efficacy after oral administration in the rat ferric chloride model. ACT-281959 entered clinical studies in healthy volunteers. ACT-281959 had been in phase I clinical trials by Actelion for the treatment of thrombosis. But there is no development reported for this study recently.
Originator
Approval Year
Sample Use Guides
The study had a double-blind, randomized, ascending single-dose design with an oral formulation F1 (i.e., ACT-281959 or placebo) (Part I) and an open-label, randomized, 3-period, crossover design comparing exploratory formulations of ACT-281959 (F2) 70 mg and ACT-246475 (dF) 50 mg to F1 70 mg (Part II). In Part I, doses up to 1,000 mg were tested in 40 healthy subjects.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:29:46 GMT 2023
by
admin
on
Sat Dec 16 10:29:46 GMT 2023
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| Record UNII |
6DPK7O4PR7
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| Record Status |
Validated (UNII)
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TARGET -> INHIBITOR |
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| Related Record | Type | Details | ||
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PRODRUG -> METABOLITE ACTIVE |
IN-VITRO
Scientific Literature
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ACTIVE MOIETY |
Official Title: A Single-center, Double-blind, Randomized, Placebo-controlled, Single-ascending Oral Dose and Food Interaction Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ACT-281959 / ACT-246475 in Healthy Male Subjects
Purpose: Study Part I is a single-ascending dose study. Healthy male subjects to be included in the study and randomized in 6 dose groups, Groups A-F (8 subjects per group). Of the 8 subjects per group, 6 subjects receive the investigational drug and 2 subjects receive matching placebo. Study Part II is a 3-period, crossover, single dose study. Nine healthy male subjects to be enrolled in one group (Group G). Each subject to receive 2 different formulations of the prodrug and one formulation of the active drug in a randomized sequence.
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