Delving into the Latest Updates on Taranabant with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Taranabant (USAN/INN)

Target

CB1R

Mechanism

CB1 inverse agonists(Cannabinoid CB1 receptor inverse agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Obesity

Inactive Indication

Behavioural disordersSmokingSmoking Cessation+ [2]

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization

Merck Research Laboratories Massachusetts LLC

Inactive Organization

Merck GmbH

Merck Sharp & Dohme Corp.Patheon Softgels, Inc. (North Carolina)

+ [1]

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure

Molecular FormulaC27H25ClF3N3O2

InChIKeyQLYKJCMUNUWAGO-GAJHUEQPSA-N

CAS Registry701977-09-5

A Phase IIb/III Randomized, Placebo-Controlled Clinical Trial to Study the Safety and Efficacy of Taranabant (MK-0364) in Overweight and Obese Patients With Type 2 Diabetes Mellitus (T2DM) Followed by a 1-Year Extension - MK-0364: One-Year Weight-Loss in Overweight and Obese Patients with T2DM with 1-Year Extension

Start Date22 Nov 2006

Sponsor / Collaborator-

EUCTR2006-004534-32-DE / Not yet recruitingNot Applicable

A Phase III Randomized, Placebo-controlled Clinical Trial to Study the Safety and Efficacy of Taranabant (MK-0364) in Obese Patients and in Overweight Patients with Obesity-related Co-morbidities, Followed by a 1- Year Extension - A 2-YEAR STUDY OF MK-0364 IN OBESE/OVERWEIGHT PATIENTS

Start Date17 Nov 2006

Sponsor / Collaborator

Merck & Co., Inc.

EUCTR2006-004366-14-SE / Not yet recruitingNot Applicable

Full title of the trial A Study to Assess the Efficacy and Tolerability of MK-0364 in Maintaining Weight Loss Induced by Diet in Obese Patients Followed by a 1-Year Extension - A Weight Maintenance Study of MK-0364 PN012 with 1-year Extension

Start Date13 Nov 2006

Sponsor / Collaborator-

100 Clinical Results associated with Taranabant

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100 Translational Medicine associated with Taranabant

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100 Patents (Medical) associated with Taranabant

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59

Literatures (Medical) associated with Taranabant

01 Jun 2024·The Lancet Diabetes & Endocrinology

Sex, race, and BMI in clinical trials of medications for obesity over the past three decades: a systematic review

Review

Author: le Roux, Carel W ; Alsaqaaby, Moath S ; Pournaras, Dimitri J ; Cooney, Sarah

Medications for obesity have been studied in various populations over the past three decades. We aimed to quantify the baseline demographic characteristics of BMI, sex, age, and race in randomised clinical trials (RCTs) across three decades to establish whether the population studied is representative of the global population affected by the disease. Clinical trials of 12 medications for obesity (ie, orlistat, naltrexone-bupropion, topiramate-phentermine, liraglutide, semaglutide, lorcaserin, sibutramine, rimonabant, taranabant, tirzepatide, retatrutide, and orforglipron) published from Jan 20, 1999, to Nov 12, 2023, were assessed through a systematic review for methodological quality and baseline demographic characteristics. 246 RCTs were included, involving 139 566 participants with or without type 2 diabetes. Most trials over-recruited White, female participants aged 40 years or older with class 1 (30·0-34·9 kg/m²) and class 2 (35·0-39·9 kg/m²) obesity; older participants, those with class 3 (≥40·0 kg/m²) obesity, non-White participants, and male participants were under-recruited. Our systematic review suggests that future trials need to recruit traditionally under-represented populations to allow for accurate measures of efficacy of medications for obesity, enabling more informed decisions by clinicians. It is also hoped that these data will help to refine trial recruitment strategies to ensure that future studies are relevant to the population affected by obesity.

01 Jan 2023·Bioorganic Chemistry

Modulating the affinity and signaling bias of cannabinoid receptor 1 antagonists

Article

Author: Chen, Yan-Fu ; Hsiao, Wen-Chi ; Song, Jen-Shin ; Hsin, Kun-Yi ; Shia, Kak-Shan ; Wu, Zhong-Wei ; Tsai, Chia-Hua ; Chen, Pei-Hsuan ; Yeh, Yen-Nan ; Chang, Chun-Ping ; Hung, Ming-Shiu

Cannabinoid receptor 1 (CB1) is a G protein-coupled receptor and a therapeutic target for metabolic disorders. Numerous CB1 antagonists have been developed, but their functional selectivities and bias towards G protein or β-arrestin signaling have not been systemically characterized. In this study, we analyzed the binding affinities and downstream signaling of two series of pyrazole derivatives bearing 1-aminopiperidine (Series I) or 4-aminothiomorpholine 1,1-dioxide (Series II) moieties, as well as the well-known CB1 antagonists rimonabant and taranabant. Analyses of the results for the Series I and II derivatives showed that minor structure modifications to their functional groups and especially the incorporation of 1-aminopiperidine or 4-aminothiomorpholine 1,1-dioxide motifs can profoundly affect their bias toward G protein or β-arrestin signaling, and that their binding affinity and functional activity can be disassociated. Docking and molecular dynamics simulations revealed that the binding modes of Series I and II antagonists differed primarily in that Series I antagonists formed an additional hydrogen bond with the receptor, whereas those in Series II formed a water bridge.

20 Jun 2019·Current Medicinal ChemistryQ2 · MEDICINE

Advances in the Understanding of the Cannabinoid Receptor 1 – Focusing on the Inverse Agonists Interactions

Q2 · MEDICINE

Review

Author: Russo, Silvana ; De Azevedo, Walter Filgueira

Background:Cannabinoid Receptor 1 (CB1) is a membrane protein prevalent in the central nervous system, whose crystallographic structure has recently been solved. Studies will be needed to investigate CB1 complexes with its ligands and its role in the development of new drugs.Objective:Our goal here is to review the studies on CB1, starting with general aspects and focusing on the recent structural studies, with emphasis on the inverse agonists bound structures.Methods: We start with a literature review, and then we describe recent studies on CB 1 crystallographic structure and docking simulations. We use this structural information to depict protein-ligand interactions. We also describe the molecular docking method to obtain complex structures of CB 1 with inverse agonists.Results:Analysis of the crystallographic structure and docking results revealed the residues responsible for the specificity of the inverse agonists for CB 1. Most of the intermolecular interactions involve hydrophobic residues, with the participation of the residues Phe 170 and Leu 359 in all complex structures investigated in the present study. For the complexes with otenabant and taranabant, we observed intermolecular hydrogen bonds involving residues His 178 (otenabant) and Thr 197 and Ser 383 (taranabant).Conclusion: Analysis of the structures involving inverse agonists and CB 1 revealed the pivotal role played by residues Phe 170 and Leu 359 in their interactions and the strong intermolecular hydrogen bonds highlighting the importance of the exploration of intermolecular interactions in the development of novel inverse agonists.

100 Deals associated with Taranabant

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External Link

KEGG	Wiki	ATC	Drug Bank
D09009	Taranabant	-	DB06624

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Obesity	Phase 2	CZ	Merck GmbH	-
Obesity	Phase 2	US	Merck GmbH	-
Obesity	Phase 2	FI	Merck GmbH	-
Obesity	Phase 2	FR	Merck GmbH	-
Obesity	Phase 2	DK	Merck GmbH	-
Obesity	Phase 2	SE	Merck GmbH	-
Obesity	Phase 2	AT	Merck GmbH	-
Obesity	Phase 2	NZ	Merck GmbH	-
Obesity	Phase 2	DE	Merck GmbH	-
Obesity	Phase 2	AU	Merck GmbH	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00430742 (Pubmed \| Diabetes Obes Metab)	Phase 3	Diabetes Mellitus, Type 2 \| Overweight \| Obesity	600	Placebo	pjtbncdssk(eqorofetic) = yblhrkgjvj xvikviwlzc (buqwxujved ) View more	-	01 Jun 2010
				Taranabant 0.5-mg	pjtbncdssk(eqorofetic) = uvdqongnut xvikviwlzc (buqwxujved ) View more
NCT00131404 (Pubmed \| Int J Psychophysiol)	Phase 3	Overweight \| Obesity	2,400	Placebo	(nghebtfidz) = lvpwxjffew ticwdrfemr (jibumnssup )	-	01 May 2010
				Taranabant 2 mg	(nghebtfidz) = zfzeflcbjd ticwdrfemr (jibumnssup )
NCT00109135 (0364-007, Pubmed \| Psychopharmacology (Berl))	Phase 2	Smoking Cessation	300	Taranabant	(vkgolgqizj) = fifiemeeoj orplimgjok (kbczfhyeik ) View more	Negative	01 Apr 2010
				Placebo	(vkgolgqizj) = bpaktczfvo orplimgjok (kbczfhyeik ) View more