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

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Showing 1291 - 1300 of 24164 results

Status:
Investigational
Source:
NCT02588105: Phase 1 Interventional Completed Advanced Solid Tumours
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT01954615: Phase 1 Interventional Completed Safety, Tolerability, Pharmacokinetics and Pharmacodynamics
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

ACT-281959 (molecular weight 850.9 g/mol), the di-ester prodrug of ACT-246475 (molecular weight 618.6 g/mol), was developed to improve absorption after oral dosing and is rapidly converted by esterases in vivo to ACT-246475 in two-steps via the formation of ACT-409100 (molecular weight 734.7 g/mol), the mono-ester prodrug. ACT-281959 is a novel potent and selective P2Y12 receptor antagonist with a wider therapeutic window. ACT-281959 showed antithrombotic efficacy after oral administration in the rat ferric chloride model. ACT-281959 entered clinical studies in healthy volunteers. ACT-281959 had been in phase I clinical trials by Actelion for the treatment of thrombosis. But there is no development reported for this study recently.
Status:
Investigational
Source:
NCT02106338: Phase 1 Interventional Completed Clostridium Difficile Infection
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



CRS-3123, also known as REP-3123, is a methionyl-tRNA synthetase inhibitor potentially for the treatment of enteric infections. CRS-3123 is in Phase 1 clinical development for the treatment of Clostridium difficile Infection (CDI). CRS-3123 is a small molecule protein synthesis inhibitor that acts on the novel target methionyl-tRNA synthetase (MetRS). REP-3123 has been shown to be active in vitro against clinical isolates of C. difficile including epidemic strains such as B1/ NAP1/027; MIC values of REP-3123 for C. difficile are typically 0.5 -- 1.0 mg/l. REP-3123 is also active against a range of clinically important aerobic Gram-positive bacteria including methicillin-susceptible and -resistant Staphylococcus aureus (MIC90 values of 0.06 and 0.25 mg/l, respectively), Streptococcus pyogenes (MIC90 0.5 mg/l) and enterococci (MIC90 32 mg/l). CRS-3123 has numerous potential advantages over current CDI therapies. In addition to being highly potent against all clinical isolates of C. difficile tested, CRS-3123 has several desirable qualities for the treatment of CDI which include: Narrow spectrum for C. difficile, which may substantially reduce the disruption of normal intestinal flora compared to current therapies; Inhibition of toxin production, potentially leading to lower morbidity and mortality; Inhibition of sporulation, potentially leading to lower rates of transmission and recurrence; A novel mechanism of action, which means that its use will not compromise the utility of systemic antibiotics while maintaining activity against pre-existing resistance mechanisms.
Status:
Investigational
Source:
NCT03332459: Phase 2 Interventional Completed Respiratory Syncytial Virus Infections
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lumicitabine (formerly called ALS-8176), a first-in-class orally administered nucleoside analogue is being developed by Alios BioPharma for the treatment of respiratory syncytial virus infections. Lumicitabine converts to plasma-circulating ALS-8112, and then to the 5'-active nucleoside triphosphate (NTP) form within host cells. Extensive and rapid RSV reduction occurred after lumicitabine treatment (EC50 = 1.79 uM), with >99% viral inhibition at 2 h after loading dose. Clinical trials of Lumicitabine for the treatment of respiratory syncytial virus infection are ongoing.
Status:
Investigational
Source:
NCT01038440: Not Applicable Interventional Completed Sudden Cardiac Death
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01449591: Phase 2 Interventional Completed Erythemato-telangiectatic Rosacea
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT01582815: Phase 2 Interventional Completed Major Depressive Disorder
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



ADX-71149 (JNJ-40411813), a phenylpiperidine-substituted pyridone, is positive allosteric modulator (PAM) metabotropic glutamate type 2 (mGlu2) receptor activity. In fed rats, JNJ-40411813 was rapidly absorbed with an absolute oral bioavailability of 31%. ADX-71149 (JNJ-40411813) demonstrates antipsychotic activity in vivo rodents experiments. ADX-71149 (JNJ-40411813) is being jointly developed by Addex Therapeutics and Janssen Pharmaceuticals, a Johnson & Johnson company, for the treatment of epilepsy. Addex Therapeutics was also developing the candidate for schizophrenia, major depressive disorder and anxiety disorders. However, development in these indications has been discontinued.
Status:
Investigational
Source:
INN:clevudine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02618616: Phase 2 Interventional Completed Psoriasis
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

PF-03893787 is potent and selective histamine H4 receptor (H4R) antagonist. It has comparable binding affinity to the human histamine H3 receptor. PF-03893787 was found to have significant affinity for the hERG channel. Novartis initiates a phase II extension trial in Atopic dermatitis. Studies exploring the utility of PF-3893787 in patients would be reported in due course, being the potential indications of asthma, pruritus, inflammatory skin diseases and pain, among others.

Showing 1291 - 1300 of 24164 results