Delving into the Latest Updates on Trimethobenzamide Hydrochloride with Synapse

This is a study with two sequential cohorts, each with three treatment periods. Single doses of PF-06649751 will be tested in this study, starting at a low dose and escalating to a dose projected to be under the current limits for drug concentration. Each cohort will aim to achieve approximately 9 completers. Primary endpoint is safety and tolerability, secondary endpoint is MDS-UPDRS part III.

Start Date01 Mar 2015

Sponsor / Collaborator

Pfizer Inc.

NCT02262767 / CompletedPhase 1

A Phase 1, Double Blind, Sponsor Open, Randomized, Placebo Controlled, Single Ascending Dose Study To Investigate The Safety, Tolerability, And Pharmacokinetics Of Pf 06649751 Co-administered With Trimethobenzamide Hydrochloride In Healthy Volunteers

This study will test the hypothesis that PF-06649751 with continuous co-administration of trimethobenzamide hydrochloride (TMB) with will be safe and well tolerated. Single doses of PF-06649751 will be tested in this study, starting at a low dose and escalating to a dose projected to be under the current limits for drug concentration.

Start Date01 Nov 2014

Sponsor / Collaborator

Pfizer Inc.

NCT01770145 / CompletedPhase 4

A Phase 4, Open-Label, Efficacy and Safety Study of Apokyn® for Rapid and Reliable Improvement of Motor Symptoms in Parkinson Disease Subjects With Delayed Onset of L-Dopa Action

This study is designed to assess the effect of APOKYN treatment in rapid and reliable improvement of motor symptoms in Parkinson's disease (PD) subjects suffering from delayed or unreliable onset of levodopa (L-dopa) action.

Start Date01 Dec 2012

Sponsor / Collaborator

MDD US Operations LLC

100 Clinical Results associated with Trimethobenzamide Hydrochloride

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100 Translational Medicine associated with Trimethobenzamide Hydrochloride

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100 Patents (Medical) associated with Trimethobenzamide Hydrochloride

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96

Literatures (Medical) associated with Trimethobenzamide Hydrochloride

19 Jan 2024·ACS Catalysis

Broad Spectrum Enantioselective Amide Bond Synthetase from Streptoalloteichus hindustanus

Article

Author: Fairlamb, Ian J. S. ; Rowlinson, Benjamin ; Tang, Qingyun ; Grogan, Gideon ; Petchey, Mark ; Burden, Thomas J.

The synthesis of amide bonds is one of the most frequently performed reactions in pharmaceutical synthesis, but the requirement for stoichiometric quantities of coupling agents and activated substrates in established methods has prompted interest in biocatalytic alternatives. Amide Bond Synthetases (ABSs) actively catalyze both the ATP-dependent adenylation of carboxylic acid substrates and their subsequent amidation using an amine nucleophile, both within the active site of the enzyme, enabling the use of only a small excess of the amine partner. We have assessed the ability of an ABS from Streptoalloteichus hindustanus (ShABS) to couple a range of carboxylic acid substrates and amines to form amine products. ShABS displayed superior activity to a previously studied ABS, McbA, and a remarkable complementary substrate specificity that included the enantioselective formation of a library of amides from racemic acid and amine coupling partners. The X-ray crystallographic structure of ShABS has permitted mutational mapping of the carboxylic acid and amine binding sites, revealing key roles for L207 and F246 in determining the enantioselectivity of the enzyme with respect to chiral acid and amine substrates. ShABS was applied to the synthesis of pharmaceutical amides, including ilepcimide, lazabemide, trimethobenzamide, and cinepazide, the last with 99% conversion and 95% isolated yield. These findings provide a blueprint for enabling a contemporary pharmaceutical synthesis of one of the most significant classes of small molecule drugs using biocatalysis.

01 Jan 2024·Clinical parkinsonism & related disorders

Apomorphine titration with and without anti-emetic pretreatment in patients with Parkinson's disease experiencing OFF episodes: A modified Delphi panel.

Article

Author: Dewey, Richard ; Lyons, Kelly E ; Hauser, Robert A ; Pagan, Fernando ; Pahwa, Rajesh ; Isaacson, Stuart H ; Lew, Mark ; Kremens, Daniel ; Ondo, William ; Kumar, Rajeev

IntroductionIn the United States (US), prophylactic treatment with the antiemetic trimethobenzamide has been used before initiating apomorphine therapy. However, US trimethobenzamide stores have been depleted, leaving uncertainty regarding whether antiemetic pretreatment is needed.MethodsThis modified Delphi panel aimed to inform circumstances when apomorphine is initiated without antiemetic pretreatment. During Round 1, a panel of 9 US movement disorder specialists rated the appropriateness of prescribing apomorphine therapy with and without antiemetic pretreatment across 192 patient scenarios and were able to review their scores in relation to other scores. During the Round 2, consensus was defined for each scenario as either strong (>75 % agreement) or moderate (66 % agreement).ResultsThere was strong consensus on 118 of 192 scenario's (97 as appropriate and 21 as inappropriate), moderate consensus on 29 scenarios, some agreement on 32 scenarios, and lack of agreement on 13 scenarios. In the absence of an antiemetic, there was strong consensus that titration schedules should be flexible and based on dose response. However, the group only reached moderate consensus on the speed of titration, highlighting the need for more systematic information on this area. In the presence of an antiemetic, panelists considered usual initial dosing and flexible titration to be appropriate in most scenarios except for when the patient is already experiencing dopaminergic adverse events.ConclusionsExperts generally reached consensus that apomorphine can usually be prescribed without antiemetic pretreatment. Recommendations described here reflect the areas of greatest agreement among a panel of experts based on current available evidence.

03 Jul 2023·ChemMedChem

Design, Synthesis, and Biological Evaluation of Histone Deacetylase Inhibitors Derived from Erianin and Its Derivatives.

Article

Author: Liu, Qingqing ; Wang, Xinyi ; Yang, Yawen ; Gou, Shaohua

Multi-target histone deacetylase (HDAC) inhibitors can be designed by introducing dominant structures of natural products to enhance activity and efficacy while avoiding the toxicity from other targets. In this study, we reported a series of novel HDAC inhibitors based on erianin and amino erianin upon pharmacophore fusion strategy. Two representative compounds, N-hydroxy-2-(2-methoxy-5- (3,4,5-trimethoxyphenethyl)phenoxy)acetamide and N-Hydroxy-8-((2-methoxy-5- (3,4,5-trimethoxyphenethyl)phenyl)amino)octanamide, possessed good inhibitory effect against five cancer cells tested (IC₅₀ =0.30-1.29 μΜ, 0.29-1.70 μΜ) with strong HDAC inhibition, and low toxicity toward L02 cells, which were selected for subsequent biological studies in PANC-1 cells. They were also found to promote the intracellular generation of reactive oxygen species, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis, which are significant for the discovery of new HDAC inhibitors.

100 Deals associated with Trimethobenzamide Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D02733	Trimethobenzamide Hydrochloride	R06AA10	DB00662

R&D Status

Approved

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Indication	Country/Location	Organization	Date
Gastroenteritis	US	Endo Operations Ltd.	12 Jul 1974
Postoperative Nausea and Vomiting	US	Endo Operations Ltd.	12 Jul 1974

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Nausea	Preclinical	BE	Pfizer Inc.	01 Nov 2014
Vomiting	Preclinical	BE	Pfizer Inc.	01 Nov 2014
Gastroenteritis	Preclinical	US	King Pharmaceuticals LLC	12 Jul 1974
Postoperative Nausea and Vomiting	Preclinical	US	King Pharmaceuticals LLC	12 Jul 1974

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01770145 (AM IMPAKT, CTgov)	Phase 4	Parkinson Disease	127	Trimethobenzamide+APOKYN+L-DOPA	wmnvchuykh(povncbfvoe) = pybzqvsakc oyytzmrzce (rfsniyunvf, vzlmxnjvqm - cbkqpctioz) View more	-	07 Sep 2015
NCT00489255 (CTgov)	Phase 4	Nausea \| Vomiting \| Parkinson Disease	117	Tigan®	mqzfxadjrh(ssbwavdcck) = ptyaffaxwe idzshglmil (gsgpzlbyvr, mjgspgvqsz - gulvrvkyeh) View more	-	20 May 2013