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Also known as: Tmc435, 923604-59-5, Tmc435350, Tmc-435, Olysio, Tmc 435

Molecular Formula

C₃₈H₄₇N₅O₇S₂

Molecular Weight

749.9 g/mol

InChI Key

JTZZSQYMACOLNN-VDWJNHBNSA-N

FDA UNII

9WS5RD66HZ

Oral HCV-PROTEASE INHIBITOR effective against hepatitis C virus (HCV) serine protease NS3/4A. It is used in the treatment of chronic hepatitis C (Antivirals) genotype 1 infection in adults with compensated liver disease, including CIRRHOSIS.

Simeprevir is a Hepatitis C Virus NS3/4A Protease Inhibitor. The mechanism of action of simeprevir is as a HCV NS3/4A Protease Inhibitor, and Cytochrome P450 3A4 Inhibitor, and P-Glycoprotein Inhibitor, and Organic Anion Transporting Polypeptide 1B1 Inhibitor, and Organic Anion Transporting Polypeptide 1B3 Inhibitor, and Cytochrome P450 1A2 Inhibitor, and Breast Cancer Resistance Protein Inhibitor, and Bile Salt Export Pump Inhibitor, and Multidrug Resistance-Associated Protein 2 Inhibitor, and Sodium Taurocholate Co-transporting Polypeptide Inhibitor.

1 2D Structure

Simeprevir

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(1R,4R,6S,7Z,15R,17R)-N-cyclopropylsulfonyl-17-[7-methoxy-8-methyl-2-(4-propan-2-yl-1,3-thiazol-2-yl)quinolin-4-yl]oxy-13-methyl-2,14-dioxo-3,13-diazatricyclo[13.3.0.04,6]octadec-7-ene-4-carboxamide

2.1.2 InChI

InChI=1S/C38H47N5O7S2/c1-21(2)30-20-51-35(40-30)29-18-32(26-13-14-31(49-5)22(3)33(26)39-29)50-24-16-27-28(17-24)36(45)43(4)15-9-7-6-8-10-23-19-38(23,41-34(27)44)37(46)42-52(47,48)25-11-12-25/h8,10,13-14,18,20-21,23-25,27-28H,6-7,9,11-12,15-17,19H2,1-5H3,(H,41,44)(H,42,46)/b10-8-/t23-,24-,27-,28-,38-/m1/s1

2.1.3 InChI Key

JTZZSQYMACOLNN-VDWJNHBNSA-N

2.1.4 Canonical SMILES

CC1=C(C=CC2=C1N=C(C=C2OC3CC4C(C3)C(=O)N(CCCCC=CC5CC5(NC4=O)C(=O)NS(=O)(=O)C6CC6)C)C7=NC(=CS7)C(C)C)OC

2.1.5 Isomeric SMILES

CC1=C(C=CC2=C1N=C(C=C2O[C@@H]3C[C@@H]4[C@@H](C3)C(=O)N(CCCC/C=C\[C@@H]5C[C@]5(NC4=O)C(=O)NS(=O)(=O)C6CC6)C)C7=NC(=CS7)C(C)C)OC

2.2 Other Identifiers

2.2.1 UNII

9WS5RD66HZ

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 435, Tmc

2. 435350, Tmc

3. N-(17-(2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diazatricyclo(13.3.0.04,6)octadec-7-ene-4-carbonyl)(cyclopropyl)sulfonamide

4. Olysio

5. Tmc 435

6. Tmc 435350

7. Tmc-435

8. Tmc-435350

9. Tmc435

10. Tmc435350

2.3.2 Depositor-Supplied Synonyms

1. Tmc435

2. 923604-59-5

3. Tmc435350

4. Tmc-435

5. Olysio

6. Tmc 435

7. Tmc 435350

8. Tmc-435350

9. Simeprevir Sodium

10. Chembl501849

11. (1r,4r,6s,7z,15r,17r)-n-cyclopropylsulfonyl-17-[7-methoxy-8-methyl-2-(4-propan-2-yl-1,3-thiazol-2-yl)quinolin-4-yl]oxy-13-methyl-2,14-dioxo-3,13-diazatricyclo[13.3.0.04,6]octadec-7-ene-4-carboxamide

12. (2r,3ar,10z,11as,12ar,14ar)-n-(cyclopropylsulfonyl)-2-({7-methoxy-8-methyl-2-[4-(1-methylethyl)-1,3-thiazol-2-yl]quinolin-4-yl}oxy)-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1h)-carboxamide

13. Simeprevir [usan]

14. 9ws5rd66hz

15. Simeprevir Sodium [jan]

16. Hcv-pi

17. Simeprevir [mi]

18. Simeprevir [inn]

19. Simeprevir [jan]

20. Simeprevir [vandf]

21. Simeprevir [who-dd]

22. Schembl826061

23. Gtpl7367

24. Dtxsid20919221

25. Chebi:134743

26. N-cyclopropylsulfonyl-[[2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methyl-4-quinolyl]oxy]-methyl-dioxo-[?]carboxamide

27. Bdbm50336504

28. S5015

29. Zinc85540268

30. Akos025401966

31. Ccg-270435

32. Ac-27651

33. As-56205

34. Tmc-00435350

35. Tmc-435, Tmc-435350

36. Us8741926, 47

37. Us8754106, 47

38. Q7517689

39. (2r,3ar,10z,11as,12ar,14ar)-n-(cyclopropylsulfonyl)-2-({7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl}oxy)-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1h)-carboxamide

40. (2r,3ar,10z,12s,13r,15ar)-n-(cyclopropylsulfonyl)-2-[[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methyl-4-quinolyl]oxy]-5-methyl-4,15-dioxo-2,3,3a,4,5,6,7,8,9,12,13,14,15,15a-tetradecahydro-12,13-methano-5,14-diaza-1h-cyclopentacyclotetradecene-13-carboxamide

41. (2r,3ar,11as,12ar,14ar)-n-(cyclopropylsulfonyl)-2-(2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-yloxy)-5-methyl-4,14-dioxo-1,2,3,3a,4,5,6,7,8,9,11a,12,12a,13,14,14a-hexadecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a-carboxamide

42. (2r,3ar,11as,12ar,14ar,z)-n-(cyclopropylsulfonyl)-2-((2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-yl)oxy)-5-methyl-4,14-dioxo-1,2,3,3a,4,5,6,7,8,9,11a,12,12a,13,14,14a-hexadecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a-carboxamide

43. (2r,3ar,11as,12ar,14ar,z)-n-(cyclopropylsulfonyl)-2-((2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-yl)oxy)-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1h)-carboxamide

44. (2r,3ar,11as,12ar,14ar,z)-n-(cyclopropylsulfonyl)-2-(2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-yloxy)-5-methyl-4,14-dioxo-1,2,3,3a,4,5,6,7,8,9,11a,12,12a,13,14,14a-hexadecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a-carboxamide

45. 1217263-04-1

46. N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0''4,6]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide

2.4 Create Date

2008-08-18

3 Chemical and Physical Properties

Molecular Formula	C₃₈H₄₇N₅O₇S₂
Molecular Weight	749.9 g/mol
XLogP3	4.8
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	10
Rotatable Bond Count	8
Exact Mass	749.29169120 g/mol
Monoisotopic Mass	749.29169120 g/mol
Topological Polar Surface Area	194 Å²
Heavy Atom Count	52
Formal Charge	0
Complexity	1490
Isotope Atom Count	0
Defined Atom Stereocenter Count	5
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	1
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Therapeutic Uses

Antiviral Agents; Protease Inhibitors

National Library of Medicine's Medical Subject Headings. Simeprevir. Online file (MeSH, 2014). Available from, as of December 18, 2014: https://www.nlm.nih.gov/mesh/2014/mesh_browser/MBrowser.html

Olysio is a hepatitis C virus (HCV) NS3/4A protease inhibitor indicated for the treatment of chronic hepatitis C (CHC) genotype 1 infection as a component of a combination antiviral treatment regimen. /Included in US product label/

NIH; DailyMed. Current Medication Information for Olysio (Simeprevir) Capsule (Revised: November 2014). Available from, as of December 31, 2014: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1816fd68-0ed7-4a37-84bb-e298c5ab6e28

Olysio monotherapy is not recommended.

Olysio combination with peginterferon alfa and ribavirin: screening patients with hepatitis C virus (HCV) genotype 1a infection for the presence of virus with the NS3 Q80K polymorphism is strongly recommended and alternative therapy should be considered if HCV genotype 1a with Q80K is detected.

Olysio is not recommended in patients who have previously failed therapy with a treatment regimen that included Olysio or other hepatitis C virus (HCV) protease inhibitors.

4.2 Drug Warning

Simeprevir contains a sulfonamide moiety. In clinical trials of simeprevir, an increased incidence of rash or photosensitivity was not observed in the 16 patients who had a history of sulfa allergy. However, data are insufficient to exclude an association between sulfa allergy and the frequency or severity of adverse reactions reported with simeprevir.

American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 807

During the 12 weeks of treatment with Olysio, dyspnea was reported in 12% of Olysio-treated subjects compared to 8% of placebo-treated subjects (all grades; pooled Phase 3 trials). All dyspnea events reported in Olysio-treated subjects were of mild or moderate severity (Grade 1 or 2). There were no Grade 3 or 4 dyspnea events reported and no subjects discontinued treatment with Olysio due to dyspnea. Sixty-one percent (61%) of dyspnea events occurred in the first 4 weeks of treatment with Olysio.

NIH; DailyMed. Current Medication Information for Olysio (Simeprevir) Capsule (Revised: November 2014). Available from, as of March 18, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1816fd68-0ed7-4a37-84bb-e298c5ab6e28

Adverse effects reported in more than 20% of patients receiving simeprevir in conjunction with peginterferon alfa and ribavirin in clinical trials and occurring with an incidence at least 3% higher than that reported in patients receiving placebo in conjunction with peginterferon alfa and ribavirin include rash (including photosensitivity), pruritus, and nausea.

American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 808

Rash has been reported in patients receiving simeprevir in conjunction with peginterferon alfa and ribavirin. Rash occurred most frequently during the first 4 weeks of treatment, but can occur at any time during the course of treatment. Rash generally was mild or moderate in severity, but severe rash and rash requiring discontinuance of the drug have been reported. Patients with mild to moderate rash should be monitored for possible progression (e.g., development of oral lesions, conjunctivitis, systemic symptoms). If rash becomes severe, simeprevir should be discontinued. Patients should be monitored until rash resolves.

American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 807

For more Drug Warnings (Complete) data for Simeprevir (12 total), please visit the HSDB record page.

4.3 Drug Indication

Olysio is indicated in combination with other medicinal products for the treatment of chronic hepatitis C (CHC) in adult patients.

For hepatitis C virus (HCV) genotype specific activity.

5 Pharmacology and Biochemistry

5.1 MeSH Pharmacological Classification

Antiviral Agents

Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly. (See all compounds classified as Antiviral Agents.)

Protease Inhibitors

Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES). (See all compounds classified as Protease Inhibitors.)

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

SIMEPREVIR

5.2.2 FDA UNII

9WS5RD66HZ

5.2.3 Pharmacological Classes

Mechanisms of Action [MoA] - Sodium Taurocholate Co-transporting Polypeptide Inhibitors

5.3 ATC Code

J05AE14

J - Antiinfectives for systemic use

J05 - Antivirals for systemic use

J05A - Direct acting antivirals

J05AP - Antivirals for treatment of hcv infections

J05AP05 - Simeprevir

5.4 Absorption, Distribution and Excretion

Simeprevir is extensively bound to plasma proteins (greater than 99.9%), primarily to albumin and, to a lesser extent, alfa 1-acid glycoprotein. Plasma protein binding is not meaningfully altered in patients with renal or hepatic impairment.

Administration of simeprevir with food to healthy subjects increased the relative bioavailability (AUC) by 61% and 69% after a high-fat, high-caloric (928 kcal) and normal-caloric (533 kcal) breakfast, respectively, and delayed the absorption by 1 hour and 1.5 hours, respectively. Due to increased bioavailability, Olysio should be administered with food. The type of food does not affect exposure to simeprevir.

Elimination of simeprevir occurs via biliary excretion. Renal clearance plays an insignificant role in its elimination. Following a single oral administration of 200 mg (14)C-simeprevir to healthy subjects, on average 91% of the total radioactivity was recovered in feces. Less than 1% of the administered dose was recovered in urine. Unchanged simeprevir in feces accounted for on average 31% of the administered dose.

In animals, simeprevir is extensively distributed to gut and liver (liver:blood ratio of 29:1 in rat) tissues. In vitro data and physiologically-based pharmacokinetic modeling and simulations indicate that hepatic uptake in humans is mediated by OATP1B1/3.

For more Absorption, Distribution and Excretion (Complete) data for Simeprevir (10 total), please visit the HSDB record page.

5.5 Metabolism/Metabolites

Following a single oral administration of 200 mg (1.3 times the recommended dosage) (14)C-simeprevir to healthy subjects, the majority of the radioactivity in plasma (mean: 83%) was accounted for by unchanged drug and a small part of the radioactivity in plasma was related to metabolites (none being major metabolites). Metabolites identified in feces were formed via oxidation at the macrocyclic moiety or aromatic moiety or both and by O-demethylation followed by oxidation.

Simeprevir is metabolized in the liver. In vitro experiments with human liver microsomes indicated that simeprevir primarily undergoes oxidative metabolism by the hepatic CYP3A system. Involvement of CYP2C8 and CYP2C19 cannot be excluded. Co-administration of Olysio with moderate or strong inhibitors of CYP3A may significantly increase the plasma exposure of simeprevir, and co-administration with moderate or strong inducers of CYP3A may significantly reduce the plasma exposure of simeprevir.

The in vitro metabolism of 14C-TMC435 was investigated in hepatocytes and liver microsomes of mouse, rat, rabbit, monkey and human. The metabolic activity reported in vitro from animals and man was low. Phase II conjugation pathways of Phase I metabolites were formed in hepatocytes. Parent TMC435 was found in much greater levels than any metabolite in vitro. More than 20 metabolites were identified. The metabolic Phase I route of highest importance were O-demethylation of unchanged drug (particularly in animals), oxidation of unchanged drug and oxidized metabolites (particularly in monkey and man) and glucuronidation was the major Phase II of oxidized metabolites (less in human). Only one human metabolite identified in vitro not seen in rat or dog was M22 (oxidized unchanged drug) but this metabolite was identified in rat (feces). In vivo data reveals that the main moiety present in plasma of rat, dog and man was parent TMC435. The major metabolites reported in vivo in plasma from animals and human were M18 and M21. O-desmethyl-TMC435 M21 was the only common circulating metabolite found in rat dog and human plasma (M21: 8% of the mean TMC435 plasma and only small traces in dogs), while M18 was common to plasma of rats and dogs but with respect to the parent compound they appeared with low concentrations (M18: between 28.9% and 12.5% in rats, with only small traces in dogs). Only traces of metabolites M18, M21 and M8 formed by O-demethylation and oxidation at the aromatic moiety were reported in dog plasma. M21 represents less than 10% of unchanged drug and also total radioactivity therefore systemic exposure to M21 was not assessed in the safety evaluation studies. M21 did not appear to accumulate in man. In bile from rats, moderately high levels of parent compound were reported (0.11 to 17.2%). TMC435 metabolites in this matrix were formed mainly by hydroxylation and O-demethylation and also by glucuronidation.

European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Olysio (Simeprevir); p.19-20 (March 20, 2014). Available from, as of March 23, 2015: https://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002777/WC500167870.pdf

The most important metabolic route TMC435 in rat and dog was O-demethylation of the parent drug to M18 (12.8%- 6.4% male-female rats; 18.8% dogs). In rats other metabolites were formed by oxidation of M18 and oxidation of unchanged drug. In dogs, further oxidation of M18 to M14 and M8, and of the unchanged drug to M21, M16 and M11 were also reported as minor routes. The human metabolism profile suggests that TMC435 is mainly metabolized by two main routes, (1) oxidation of unchanged drug, either at the macrocyclic moiety (M27, M21 and M22), or at the aromatic moiety (M26 and M16), or both (M23, M24, M25 and M11) and (2) the O-demethylation of unchanged drug to M18, followed by oxidation on the macrocyclic moiety to M14 and by oxidation on the aromatic moiety to M5, appears to be the secondary metabolic pathway in man. M21 and M22 were the most important metabolites in human faeces. Other relevant metabolites (1% of the dose) were M11, M16, M27 and M18. All metabolites detected in human feces were detected in vitro and/or in vivo in rat and/or dog feces. The main CYP enzymes involved in TMC435 metabolism were CYP3A enzymes although in vitro data suggests the involvement of CYP2C8 and CYP2C19.

European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Olysio (Simeprevir); p.20 (March 20, 2014). Available from, as of March 23, 2015: https://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002777/WC500167870.pdf

5.6 Biological Half-Life

The half-life was variable among species accounting to 4.0 hr in rats, 3.7 hr in rabbits and dogs and 5 to 6 hr in Rhesus and Cynomolgus monkeys.

European Medicines Agency (EMA), Committee for Medicinal Products for Human Use (CHMP), European Public Assessment Report (EPAR): Olysio (Simeprevir); p.19 (March 20, 2014). Available from, as of March 23, 2015: https://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002777/WC500167870.pdf

The terminal elimination half-life of simeprevir was 10 to 13 hours in hepatitis C virus (HCV)-uninfected subjects and 41 hours in HCV-infected subjects receiving 200 mg (1.3 times the recommended dosage) of simeprevir.

5.7 Mechanism of Action

Simeprevir sodium is a selective hepatitis C virus (HCV) nonstructural 3/4A (NS3/4A) protease inhibitor (PI). The drug is a direct-acting antiviral (DAA) with activity against HCV. Simeprevir binds noncovalently to the active site of HCV NS3/4A protease, thereby blocking enzyme activity essential for viral replication (i.e., cleavage of the HCV-encoded polyprotein at the NS3/NS4A, NS4A/NS4B, NS4A/NS5A, and NS5A/NS5B junctions). In vitro studies using biochemical and cell-based replicon assays indicate that simeprevir has potent activity against HCV genotypes 1a and 1b1 5 8 9 and has some activity against HCV genotypes 2, 4, 5, and 6 (not genotype 3).

American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 809

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Beijing Mesochem Technology

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DEAFARMA

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Haoyuan Chemexpress Co.Ltd

China

Antibody Engineering

Not Confirmed

Haoyuan Chemexpress Co.Ltd

China

Antibody Engineering

Not Confirmed

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Simeprevir

About the Company : Haoyuan Chemexpress Co., Ltd., located in Shanghai Zhangjiang Biomedical Base, is a high-tech company specializing in customized chemical synthesis and R&D of pharmaceutical interm...

Haoyuan Chemexpress Co., Ltd., located in Shanghai Zhangjiang Biomedical Base, is a high-tech company specializing in customized chemical synthesis and R&D of pharmaceutical intermediates and new drugs. The company is mainly engaged in customized synthesis of complex small molecule frameworks and pharmaceutical intermediates, and independent R&D of innovative new drugs; and provides services of production technology improvement and consigned new drug development for pharmaceutical enterprises. Haoyuan Chemexpress is committed to researching and developing APIs and pharmaceutical intermediates with high synthesis technology barriers and difficulties and high added value, and also focuses on the synthesis of chiral compounds.

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