U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1001 - 1010 of 39585 results

Status:
Investigational
Source:
INN:epaminurad [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


(3,5-DIBROMO-4-HYDROXYPHENYL)(2,3-DIHYDRO-4H-PYRIDO[4,3-B][1,4]OXAZIN-4-YL)METHANONE (UR-1102/URC-1022) is currently under development for the management of hyperuricaemia in gout. It is a selective URAT1 inhibitor with Ki of 57 nM showing higher uricosuric effects than benzbromarone in monkeys with potentially lower mitochondrial toxicity which is supposed to be related to hepatotoxicity. There is also a probable inhibition of OAT1 and OAT3. UR-1102, which is derived from the chemical structure of benzbromarone, was designed to not only improve URAT1 selectivity and solubility but also to avoid the hepatic toxicity concern of benzbromarone, which is known to be associated with hepatic injury and to have the potential to cause fulminant hepatitis in humans. The results of two phase II trials presented at the 2017 ACR meeting suggested a high potency for reducing SU levels with a good safety profile on a short follow-up. No phase III trial has been registered so far.
Status:
Investigational
Source:
INN:myrtecaine
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Status:
Investigational
Source:
INN:becondogrel [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03512171: Phase 1 Interventional Completed Healthy Adults
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03212430: Phase 1 Interventional Completed Headache
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Kynurenine is a metabolite of the amino acid L-tryptophan used in the production of niacin. Kynurenine is synthesized by the enzyme tryptophan dioxygenase, which is made primarily but not exclusively in the liver, and indoleamine 2,3-dioxygenase, which is made in many tissues in response to immune activation. Kynurenine and its further breakdown products carry out diverse biological functions, including dilating blood vessels during inflammation and regulating the immune response. Evidence suggests that increased kynurenine production may precipitate depressive symptoms associated with interferon treatment for hepatitis C. Cognitive deficits in schizophrenia are associated with imbalances in the enzymes that break down kynurenine. Kynurenine production is increased in Alzheimer's disease and cardiovascular disease where its metabolites are associated with cognitive deficits and depressive symptoms.
Status:
Investigational
Source:
NCT04604652: Phase 2 Interventional Completed Primary Biliary Cholangitis
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03301896: Phase 1 Interventional Terminated Solid Tumors
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04341454: Phase 3 Interventional Completed Acute Gastritis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03817684: Phase 2 Interventional Completed Alzheimer's Disease
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04328077: Phase 2 Interventional Completed NASH - Nonalcoholic Steatohepatitis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Showing 1001 - 1010 of 39585 results