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TD-4208; GSK-1160724;[1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] N-(2-phenylphenyl)carbamate

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ACTIVE PHARMA INGREDIENTS

14 API Suppliers, 6 USDMF, 1 EU WC, 5 NDC API, 11 Listed Suppliers, $ API Reference Price

14 API Suppliers
6 USDMF
1 EU WC
5 NDC API
11 Listed Suppliers
$ API Reference Price

DEVELOPMENTS

3 Drugs in Development

3 Drugs in Development

INTERMEDIATES

2 Intermediates Suppliers

2 Intermediates Suppliers

FINISHED DOSAGE FORMULATIONS

2 FDF Dossiers, 1 FDA Orange Book, 1 Listed Dossiers

2 FDF Dossiers
1 FDA Orange Book
1 Listed Dossiers

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1 DATA COMPILATION #PharmaFlow, 12 NEWS #PharmaBuzz

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GLOBAL SALES INFORMATION

1 US Medicaid Prescriptions, 2 Annual Reports

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1 US Medicaid Prescriptions
2 Annual Reports

MARKET PLACE

8 APIs

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8 APIs

PATENTS & EXCLUSIVITIES

20 US Patents

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20 US Patents

Inke Revefenacin

Synopsis

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US Medicaid (USD)

2,154,000

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423

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Chemistry

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Also known as: 864750-70-9, Td-4208, Yupelri, Gsk-1160724, Gsk1160724, Revefenacin [inn]

Molecular Formula

C₃₅H₄₃N₅O₄

Molecular Weight

597.7 g/mol

InChI Key

FYDWDCIFZSGNBU-UHFFFAOYSA-N

FDA UNII

G2AE2VE07O

Revefenacin is a novel biphenyl carbamate tertiary amine agent that belongs to the family of the long-acting muscarinic antagonists (LABA). The labile primary amide in the structure produces a "soft-drug" site that allows rapid systemic clearance and minimizing of the systemically mediated adverse reactions. The LABA group falls into a parent category known as long-acting inhaled bronchodilators and this type of agents are recommended as a maintenance therapy for chronic obstructive pulmonary disease (COPD). From the LABA group, revefenacin is the first once-daily nebulized LAMA treatment. It was developed by Theravance Biopharma and FDA approved on November 9, 2018.

Revefenacin is an Anticholinergic. The mechanism of action of revefenacin is as a Cholinergic Antagonist.

1 2D Structure

Revefenacin

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

[1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] N-(2-phenylphenyl)carbamate

2.1.2 InChI

InChI=1S/C35H43N5O4/c1-38(34(42)29-13-11-26(12-14-29)25-40-19-15-28(16-20-40)33(36)41)23-24-39-21-17-30(18-22-39)44-35(43)37-32-10-6-5-9-31(32)27-7-3-2-4-8-27/h2-14,28,30H,15-25H2,1H3,(H2,36,41)(H,37,43)

2.1.3 InChI Key

FYDWDCIFZSGNBU-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CN(CCN1CCC(CC1)OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)C(=O)C4=CC=C(C=C4)CN5CCC(CC5)C(=O)N

2.2 Other Identifiers

2.2.1 UNII

G2AE2VE07O

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Biphenyl-2-ylcarbamic Acid 1-(2-((4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl)methylamino)ethyl)piperidin-4-yl Ester

2. Td-4208

3. Yupelri

2.3.2 Depositor-Supplied Synonyms

1. 864750-70-9

2. Td-4208

3. Yupelri

4. Gsk-1160724

5. Gsk1160724

6. Revefenacin [inn]

7. Revefenacin [who-dd]

8. G2ae2ve07o

9. 864750-70-9 (free Base)

10. [1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] N-(2-phenylphenyl)carbamate

11. 1-(2-(4-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl N-((1,1'-biphenyl)-2-yl)carbamate

12. 1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate

13. Biphenyl-2-ylcarbamic Acid, 1-(2-((4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl)methylamino)ethyl)piperidin-4-yl Ester

14. Carbamic Acid, N-(1,1'-biphenyl)-2-yl-, 1-(2-((4-((4-(aminocarbonyl)-1-piperidinyl)methyl)benzoyl)methylamino)ethyl)-4-piperidinyl Ester

15. Td-4208; Gsk-1160724;[1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] N-(2-phenylphenyl)carbamate

16. Revefenacin [mi]

17. Revefenacin (usan/inn)

18. Revefenacin [usan:inn]

19. Revefenacin [usan]

20. Unii-g2ae2ve07o

21. Revefenacin;gsk1160724

22. Schembl356480

23. Chembl3833319

24. Gtpl10129

25. Revefenacin [orange Book]

26. Dtxsid701027775

27. Hms3886k17

28. Amy16789

29. Bcp15793

30. Ex-a1722

31. S5258

32. Td4208

33. Akos037649398

34. Ccg-270187

35. Cs-7743

36. Db11855

37. Sb17262

38. Bs-18189

39. Hy-15851

40. Revefenacin; Td-4208; Gsk-1160724

41. D10978

42. A903445

43. Q27278649

44. Revefenacin; Td 4208; Td4208; Gsk-1160724; Gsk1160724; Gsk 1160724

45. 1-(2-(4-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate

46. 1211931-83-7

47. Td-4208; Td 4208; Td4208; Gsk-1160724; Gsk1160724;1-(2-(4-((4-carbamoylpiperidin-1-yl)methyl)-n-methylbenzamido)ethyl)piperidin-4-yl N-((1,1'-biphenyl)-2-yl)carbamate

2.4 Create Date

2006-10-26

3 Chemical and Physical Properties

Molecular Formula	C₃₅H₄₃N₅O₄
Molecular Weight	597.7 g/mol
XLogP3	4.1
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	11
Exact Mass	597.33150487 g/mol
Monoisotopic Mass	597.33150487 g/mol
Topological Polar Surface Area	108 Å²
Heavy Atom Count	44
Formal Charge	0
Complexity	918
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

Revefenacin is indicated as an inhalation solution for the maintenance treatment of patients with chronic obstructive pulmonary disease (COPD). COPD is a growing disease being the third leading cause of death in the US. This disease is characterized by not fully reversible airflow limitation.

FDA Label

5 Pharmacology and Biochemistry

5.1 Pharmacology

Revefenacin has been reported to produce a sustained, long-acting bronchodilation with lower anti-muscarinic-related side effects. In clinical trials, revefenacin demonstrated to be of a long duration of action and low systemic exposure in patients with COPD. Also, it was reported that a dose of 88 mcg can produce a clinically effective bronchodilation measured by through forced expiratory volume in 1s and serial spirometric assessments. In placebo-controlled trials, revefenacin showed a decrease in the use of albuterol rescue inhalers and sustained increases in the peak expiratory flow rate that reached a steady state at a maximum in day 7. As well, there was a reported superior lung selectivity index when compared with other LABAs such as glycopyrronium and tiotropium which produced a decreased sialagogue effect.

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

REVEFENACIN

5.2.2 FDA UNII

G2AE2VE07O

5.2.3 Pharmacological Classes

Cholinergic Antagonists [MoA]; Anticholinergic [EPC]

5.3 ATC Code

R - Respiratory system

R03 - Drugs for obstructive airway diseases

R03B - Other drugs for obstructive airway diseases, inhalants

R03BB - Anticholinergics

R03BB08 - Revefenacin

5.4 Absorption, Distribution and Excretion

Absorption

In pharmacokinetic studies, revefenacin was absorbed very rapidly and presented a linear increase in plasma exposure with Cmax, tmax and AUC that ranged between 0.02-0.15 ng/ml, 0.48-0.51 hours and 0.03-0.36 ng.h/ml, respectively. The bioaccumulation of revefenacin was very limited and the steady-state was achieved by day 7.

Route of Elimination

After reaching maximum concentration, revefenacin concentrations decline in a biphasic manner. This elimination kinetics is observed by a rapid declining plasma concentration followed by a slow apparent bi-exponential elimination. Renal elimination of revefenacin is limited and it presents a mean cumulative amount excreted in urine as the unchanged drug of < 0.2% of the administered dose. Following intravenous revefenacin administration, 54% of the dose is recovered in feces and 27% was recovered in urine which confirms a high hepatobiliary processing.

Volume of Distribution

After intravenous administration of revefenacin, the reported volume of distribution is 218 L which suggests an extensive distribution to the tissues.

Clearance

The renal clearance of revefenacin is negligible and thus, the clearance rate is not a major parameter for this drug.

5.5 Metabolism/Metabolites

Revefenacin presents a high metabolic liability producing a rapid metabolic turnover after being distributed from the lung. This metabolic process is done primarily via enzymatic hydrolysis via CYP2D6 to its major hydrolytic metabolite THRX-195518.

5.6 Biological Half-Life

The apparent terminal half-life of a dose of 350 mcg of revefenacin was 22.3-70 hours.

5.7 Mechanism of Action

Revefenacin is an inhaled bronchodilator muscarinic antagonist with a long-acting bronchodilation activity. It has been shown to present a high affinity and behaved as a competitive antagonist of the five muscarinic cholinergic receptors. Studies have indicated that revefenacin dissociates significantly slower from the muscarinic receptor M3 (hM3) when compared to the receptor M2 (hM2) which indicates a kinetic selectivity for this subtype. This competitive antagonism produces a suppressive action of the acetylcholine-evoked calcium mobilization and contractile responses in the airway tissue. Lastly, due to the duration of the bronchodilation, revefenacin is considered a long-acting muscarinic antagonist which allows it to be dosed once daily. This response is very important for the therapy of COPD as the main goal is the reduce the frequency and severity of exacerbations which are normally driven by the presence of elevated cholinergic bronchoconstrictor tone mediated by muscarinic receptors on parasympathetic ganglia and airway smooth muscle. Hence, the activity of revefenacin produces a potent and long-lasting protection against the bronchoconstrictor response to acetylcholine or methacholine.

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01

Inke S.A

Spain

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Transo-Pharm USA LLC

U.S.A

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2024 ISPE Annual Meeting

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TransoPharm USA works in the Sourcing and Management of Active Pharmaceutical Ingredients.

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Hubei Gedian Humanwell Pharmaceuti...

China

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CPhI India 2024

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Hubei Gedian Humanwell focuses on R&D, production, & sales of fertility regulation drugs & steroidal APIs.

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Medichem S.A

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Shandong Loncom Pharmaceutical

China

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2024 ISPE Annual Meeting

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Shandong Loncom is an R&D-focused manufacturer of Anti-cancer APIs.

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Aurobindo Pharma Limited

India

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2024 ISPE Annual Meeting

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Cipla

India

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Mankind Pharma

India

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MSN Laboratories

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USDMF

01

Inke Sa

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Inke S.A: APIs manufacturing plant.

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Spain

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Revefenacin Trihydrate

GDUFA

DMF Review : Complete

Rev. Date : 2022-09-01

Pay. Date : 2022-03-17

DMF Number : 36481

Submission : 2022-07-27

Status : Active

Type : II

02

Medichem Manufacturing Malta Ltd

Spain

CPhI India 2024

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Medichem is a vertically integrated pharmaceutical company specializing in the development & manufacturing of APIs & FDFs.

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Spain

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Revefenacin

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DMF Review : Complete

Rev. Date : 2022-05-10

Pay. Date : 2022-04-11

DMF Number : 36861

Submission : 2022-04-19

Status : Active

Type : II

03

Apitoria Pharma Private Ltd

India

2024 ISPE Annual Meeting

Not Confirmed

04

Cipla Ltd

India

2024 ISPE Annual Meeting

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Mankind Pharma Ltd

India

2024 ISPE Annual Meeting

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Msn Laboratories Private Ltd

India

2024 ISPE Annual Meeting

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Listed Suppliers

01

Inke S.A

Spain

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Revefenacin

About the Company : Inke S.A., is focused since 1980 in the development and manufacture of the highest quality Active Pharmaceutical Ingredients (APIs) with complex synthesis processes for diverse the...

Inke S.A., is focused since 1980 in the development and manufacture of the highest quality Active Pharmaceutical Ingredients (APIs) with complex synthesis processes for diverse therapeutic areas, but mainly for use in Respiratory. Inke has been successfully inspected by every major global authority for a wide array of products (last inspection on behalf of US-FDA was in 2023). For the last two decades, the company has made strong strides to become a prestige provider of respiratory APIs for inhalation.

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Transo-Pharm USA LLC

U.S.A

Fall Technical Meeting

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Revefenacin

About the Company : Transo-Pharm, a fully licensed and certified distributor, specializes in pharmaceutical components for the health and veterinary industries. It offers support to clients throughout...

Transo-Pharm, a fully licensed and certified distributor, specializes in pharmaceutical components for the health and veterinary industries. It offers support to clients throughout the entire API life cycle, from product development through sales. Transo-Pharm serves as a sourcing and regulatory marketing agent for API manufacturers. It aids clients in establishing DMFs and provides GMP consulting. With a dedicated regulatory department, a warehouse, proprietary IPs for API processes, and partnerships with laboratories, Transo-Pharm offers a wide range of services. It operates from its offices in Shanghai, Hong Kong, Singapore, and the US.

03

Hubei Gedian Humanwell Pharmaceutic...

China

CPhI India 2024

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Hubei Gedian Humanwell focuses on R&D, production, & sales of fertility regulation drugs & steroidal APIs.

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China

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Revefenacin

About the Company : Hubei Gedian Humanwell Pharmaceutical Co., Ltd. is a modern high-tech pharmaceutical company with a focus on the research and development, production, and sales of fertility regula...

Hubei Gedian Humanwell Pharmaceutical Co., Ltd. is a modern high-tech pharmaceutical company with a focus on the research and development, production, and sales of fertility regulation drugs and steroidal APIs. It operates as a wholly-owned subsidiary of Humanwell Healthcare Group (Stock Code: 600079), one of the leading pharmaceutical conglomerates in China. The company operates two APIs manufacturing sites, one formulation factory, and one excipients factory, showcasing its commitment to integrating the reproductive health industry chain from raw materials and active pharmaceutical ingredients (APIs) to finished dosage forms.

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Medichem S.A

Spain

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Medichem is a vertically integrated pharmaceutical company specializing in the development & manufacturing of APIs & FDFs.

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Revefenacin

About the Company : Medichem is an indepently-owned company based in Barcelona. Founded in 1972 and with more than 45 years, Medichem has been engaged in the process development and manufacture of Act...

Medichem is an indepently-owned company based in Barcelona. Founded in 1972 and with more than 45 years, Medichem has been engaged in the process development and manufacture of Active Pharmaceutical Ingredients (APIs), including Highly Potent. In 2016, Medichem merged with Combino Pharm, which is devoted to the development and manufacture (licensing) of Finished Dosage Forms. With this merger, Medichem has become a vertically integrated pharmaceutical company which can offer a complete range of products and services for the pharmaceutical industry with the highest standards of quality, operational excellence and environment respect.

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Shandong Loncom Pharmaceutical

China

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Revefenacin

About the Company : Established in May 2012, Shandong Loncom Pharmaceutical operates as a fully owned subsidiary of Shandong Bestcomm Pharmaceutical Co., Ltd. Situated in the Qihe Economic Development...

Established in May 2012, Shandong Loncom Pharmaceutical operates as a fully owned subsidiary of Shandong Bestcomm Pharmaceutical Co., Ltd. Situated in the Qihe Economic Development Zone, Shandong Province, Shandong Loncom has operational API pilot tests and production bases adhering to international standards. With 13 production lines dedicated to oral solid preparations, oral liquid preparations and API, it is actively expanding its preparation workshops for small-volume injections, soft capsules, eye drops, topical medicines and innovative drug R&D centres.