Delving into the Latest Updates on Tepilamide fumarate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Methyl hydrogen fumarate prodrug, Tepilamide fumarate (USAN/INN)

+ [2]

Target

Nrf2

Mechanism

Nrf2 stimulants(Nuclear factor erythroid 2-related factor 2 stimulants)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal DiseasesNervous System Diseases+ [2]

Active Indication-

Inactive Indication

Multiple SclerosisParkinson DiseasePlaque psoriasis

Originator Organization

XenoPort, Inc.

Active Organization-

Inactive Organization

XenoPort, Inc.Dr. Reddy's Laboratories Ltd. (Russia)Dr. Reddys Laboratories Tennessee LLC

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC11H17NO5

InChIKeyAKUGRXRLHCCENI-VOTSOKGWSA-N

CAS Registry1208229-58-6

The study objectives are the following:
To evaluate the efficacy of 3 doses of XP23829 compared to placebo for the treatment of moderate-to-severe chronic plaque-type psoriasis.
To evaluate the safety and tolerability of XP23829 in subjects with psoriasis.
To evaluate the pharmacodynamics (PD) of XP23829 through immunological analysis of peripheral blood samples.

Start Date01 Jun 2014

Sponsor / Collaborator

Dr. Reddy's Laboratories Ltd. (Russia)

[+1]

100 Clinical Results associated with Tepilamide fumarate

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100 Translational Medicine associated with Tepilamide fumarate

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100 Patents (Medical) associated with Tepilamide fumarate

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5

Literatures (Medical) associated with Tepilamide fumarate

01 Sep 2022·Environmental Research

O- and F-doped porous carbon bifunctional catalyst derived from polyvinylidene fluoride for sulfamerazine removal in the metal-free electro-Fenton process

Article

Author: Cao, WenXing ; Li, Yang ; Zuo, XiaoJun

Heteroatom-doped carbon materials can effectively activate H₂O₂ into •OH during the metal-free electro-Fenton (EF) process. However, information on bifunctional catalysts for the simultaneous generation and activation of H₂O₂ is scarce. In this study, O- and F-doped porous carbon cathode materials (PPCs) were prepared by the direct carbonization of polyvinylidene fluoride (PVDF) for sulfamerazine (SMR) removal in a metal-free EF process. The porous structure and chemical composition of the PPCs were regulated by the carbonization temperature. PPC-6 (carbonized at 600 °C) exhibited optimal electrocatalytic performance in terms of electrochemical H₂O₂ generation and activation owing to its high specific surface area, mesoporous structure, and optimum fractions of doped O and F. Excellent performance of the 2e^- oxygen reduction reaction was found with an H₂O₂ selectivity of 93.5% and an average electron transfer number of 2.13. An H₂O₂ accumulative concentration of 103.9 mg/L and an SMR removal efficiency of 90.1% were achieved during the metal-free EF process. PPC-6 was able to stably remove SMR over five consecutive cycles, retaining 92.6% of its original performance. Quantitative structure-activity relationship analysis revealed that doped oxygen functional groups contributed substantially to H₂O₂ generation, and semi-ionic C-F bonds with high electronegativity were the cause of the activation of H₂O₂ to •OH. These findings suggest that the PVDF-derived carbonaceous catalysts are feasible and desirable for metal-free EF processes.

01 Jan 2022·The Journal of clinical and aesthetic dermatology

Tepilamide Fumarate (PPC-06) Extended Release Tablets in Patients with Moderate-to-Severe Plaque Psoriasis: Safety and Efficacy Results from the Randomized, Double-blind, Placebo-controlled AFFIRM Study.

Article

Author: Reich, Kristian ; Mrowietz, Ulrich ; Munjal, Sagar ; Kircik, Leon ; Shenoy, Srinivas ; Lebwohl, Mark

ObjectiveSafe, effective, long-term oral therapies are needed for plaque psoriasis. This study aimed to assess the safety and effectiveness of tepilamide fumarate (a fumaric acid ester) extended-release tablets.MethodsThis Phase IIb, randomized, double-blind, placebo-controlled, 24-week, multicenter study treated adults with moderate-to-severe plaque psoriasis with tepilamide fumarate 400 mg once (QD) or twice daily (BID), 600 mg BID, or placebo. Coprimary endpoints were the proportion of patients achieving ≥75% reduction in the Psoriasis Area and Severity Index (PASI-75) and Investigator's Global Assessment (IGA) of clear or almost clear (≥2 points' reduction).ResultsA total of 426 patients were randomized (mean age 49.6 [±13.0] years). There was a ≥75% PASI reduction in 39.7%, 47.2%, 44.3%, and 20.0% in the 400 mg QD, 400 mg BID, 600 mg BID, and placebo groups, respectively; IGA treatment success was 35.7%, 41.4%, 44.4%, and 22.0%, respectively. Between 50%-66% of tepilamide fumarate and 48% of placebo patients experienced ≥1 treatment-emergent adverse event. Gastrointestinal intolerance (20%-42%), infection (6%-18%), and decreased lymphocyte count (4%-9%) were more common with tepilamide fumarate.LimitationsHigh placebo response somewhat limits the utility of these findings.ConclusionPatients with moderate-to-severe plaque psoriasis treated with oral tepilamide fumarate demonstrated positive response.

01 Feb 2001·Transplantation ProceedingsQ4 · MEDICINE

Methyl hydrogen fumarate inhibits acute and chronic rejection in rat kidney transplantation models

Q4 · MEDICINE

Article

Author: J Lutz ; M Lehmann ; R.K Joshi ; J Brock ; H.P Strebel ; K Asadullah ; H.-D Volk ; K Risch

The immunosuppressive effect of Me hydrogen fumarate (MHF) using calcium methylfumarate (CaMF) in rat transplantation models of acute (AR) and chronic rejection (CR) was studied.Orthotop kidney transplantation (T_x) was combined with contralateral nephrectomy using the strain combination WF(RT1u) to BDIX (RT1dv1) (AR model) and F344 (RT1lv1) to LEW (RT1l) (CR model).Recipients were treated per os (stomach tube) prophylactically or therapeutically with 33.3 mg/kg per day CaMF.In the CR model, rats were treated also with 1.5 mg/kg cyclosporin A for 10 days.Anal. of the immune state of rats surviving the observation period of 100 days by donor specific retransplantation showed that the tested immunosuppressive protocol did not induce tolerance.Comparing two different schedules of CaMF-treatment in the CR model F344 to LEW, prophylactic administration resulted in more effective inhibition of CR than seen for the therapeutical administration.The clin. onset of chronic graft injury about 12 wk after T_x is preceded by rising cellular graft infiltration by macrophages from week eight which peaks between week 12 and 16.

100 Deals associated with Tepilamide fumarate

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External Link

KEGG	Wiki	ATC	Drug Bank
D11335	-	-	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Plaque psoriasis	NDA/BLA	US	XenoPort, Inc.	01 Jun 2014
Plaque psoriasis	NDA/BLA	US	Dr. Reddy's Laboratories Ltd. (Russia)	01 Jun 2014
Multiple Sclerosis	Phase 2	US	XenoPort, Inc.	-
Parkinson Disease	Phase 2	US	XenoPort, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02173301 (CTgov)	Phase 2	Plaque psoriasis	200	XP23829 400 mg QD (XP23829 400 mg QD (Once Daily))	qwwajvgfxg(tlebileafe) = eughdfseos liqukbyjin (newrlgbwev, ehenpjyfru - taemisuqgr) View more	-	12 Apr 2022
				XP23829 400 mg BID (XP23829 400 mg BID (Twice Daily))	qwwajvgfxg(tlebileafe) = scbzqebsic liqukbyjin (newrlgbwev, jxnuaqrrrd - vinupypyos) View more
NCT03421197 (CTgov)	Phase 2	Plaque psoriasis	426	PPC-06 400 mg QD (PPC-06 400 mg QD)	qjxlpdaatt(mihpfyczoo) = axbgptbphy hbkqwpgzkg (swqkadfmae, lecansadmo - ylelyesbkj) View more	-	11 May 2021
				PPC-06 400 mg BID (PPC-06 400 mg BID)	qjxlpdaatt(mihpfyczoo) = lxtoelzqti hbkqwpgzkg (swqkadfmae, rzfvvmfmjt - nmppnvhebg) View more