| Stereochemistry | ABSOLUTE |
| Molecular Formula | C36H61N5O7S |
| Molecular Weight | 707.964 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]12CN([C@H](C(=O)N[C@@H](CCCC)C(=O)C(=O)NC3CC3)[C@@]1([H])C2(C)C)C(=O)[C@@H](NC(=O)NC4(CS(=O)(=O)C(C)(C)C)CCCCC4)C(C)(C)C
InChI
InChIKey=RICZEKWVNZFTNZ-LFGITCQGSA-N
InChI=1S/C36H61N5O7S/c1-10-11-15-24(27(42)30(44)37-22-16-17-22)38-29(43)26-25-23(35(25,8)9)20-41(26)31(45)28(33(2,3)4)39-32(46)40-36(18-13-12-14-19-36)21-49(47,48)34(5,6)7/h22-26,28H,10-21H2,1-9H3,(H,37,44)(H,38,43)(H2,39,40,46)/t23-,24-,25-,26-,28+/m0/s1
| Molecular Formula | C36H61N5O7S |
| Molecular Weight | 707.964 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Narlaprevir (formerly SCH 900518), a NS3 protease inhibitor is being developed by R-Pharm for the treatment of a chronic hepatitis C (genotype 1). Narlaprevir is a potent inhibitor of hepatitis C virus (HCV) NS3 protease with a Ki of 7 ± 1 nM and a 90% inhibitory concentration (IC90) of ∼28 ng/ml for HCV genotype 1 replicon in vitro. Narlaprevir successfully passed extensive pre-clinical and clinical trials in Schering-Plough Research Institute (USA) and in a variety of clinical centers of Europe, USA and Russia. Based on clinical findings R-Pharm obtained a registration certificate for Arlansa (Narlaprevir) ЛП-003622 dd 12.05.2016 issued by Ministry of Healthcare of the Russian Federation.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 6.0 nM [Ki] |
PubMed
Sample Use Guides
Narlaprevir at 200 mg was administered to 8 healthy and 8 cirrhotic subjects, and Narlaprevir at 100 mg with RTV at 100 mg was administered to 8 healthy and 8 cirrhotic subjects. In part 1 of the study, 8 patients with compensated cirrhosis and 8 matched healthy adult subjects received single doses of NVR at 200 mg with 240 ml of water after a standard breakfast. The 200-mg NVR dose was chosen since this is the intended therapeutic dose. This dose is the approved marketed dose of NVR for the treatment of CHC genotype 1 in the Russian Federation.
In part 2 of the study, 8 patients with compensated cirrhosis and 8 healthy subjects received NVR at 100 mg in combination with RTV at 100 mg with 240 ml of water after a standard breakfast.
Route of Administration:
Oral
