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

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Showing 491 - 500 of 13240 results

Status:
Investigational
Source:
INN:myfadol
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Myfadol is a phenacylpiperidine derivative patented by Tanabe Seiyaku Co., Ltd as low molecular weight non-peptide analgesic. Myfadol produces hot-plate analgesia in rodents with minimal side-effects, and when given parenterally in humans produces analgesia to experimentally-produced and postoperative pain.
Status:
Investigational
Source:
NCT03196765: Phase 1/Phase 2 Interventional Withdrawn X-Linked Adrenoleukodystrophy
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sobetirome (3,5-dimethyl-4[(4'-hydroxy-3'-isopropylbenzyl)-phenoxy] acetic acid, also known as GC-1 and QRX-431, is a member of a class of compounds known as selective thyromimetics. It was firstly developed by Thomas Scanlan’s group at the University of California-San Francisco (UCSF) in 1995. Sobetirome binds selectively to the main hepatic form of thyroid hormone (TH) receptor, TRβ1, compared to TRα1, which is principally responsible for thyrotoxic effects on heart, muscle and bone. Sobetirome also preferentially accumulates in liver. It was originally envisaged that sobetirome could be used to stimulate hepatic pathways that lower cholesterol without harmful side effects and might be used in conjunction with statins. Indeed, sobetirome progressed through preclinical animal studies and Phase I human clinical trials with excellent results and without obvious harmful side effects. Sobetirome had been in phase I clinical trials for the treatment of lipid metabolism disorders and obesity. However, this research has been discontinued.
Status:
Investigational
Source:
NCT04469023: Phase 2 Interventional Completed Patients with Insomnia
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01871428: Phase 3 Interventional Completed Diabetes Mellitus Type 2
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Aleglitazar is a dual agonist of PPARalpha/PPARgamma which was developed by Hoffmann-La Roche for the treatment of type 2 diabetes. Aleglitazar activates PPAR receptors with EC50 in nanomolar range and exerts a cardioprotective effect in vitro. The drug is currently in phase III of clinical trials.
Status:
Investigational
Source:
NCT02391480: Phase 1 Interventional Completed Cancer
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Mivebresib (ABBV-075) is a small molecule Bromodomain and Extra-Terminal motif (BET) inhibitor being studied in a Phase 1 clinical trial in patients with advanced hematologic malignancies and solid tumors. Mivebresib binds to BRD4 with a Ki of 1.5 nM. Comprehensive preclinical characterization of ABBV-075 demonstrated broad activity across cell lines and tumor models, representing a variety of hematologic malignancies and solid tumor indications. In most cancer cell lines derived from solid tumors, ABBV-075 triggers prominent G1 cell-cycle arrest without extensive apoptosis. Consistent with its broad spectrum of activities in vitro, ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia.
Status:
Investigational
Source:
NCT01487551: Phase 2 Interventional Completed Systemic Sclerosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Paquinimod is an immunomodulatory compound preventing S100A9 binding to TLR-4. It was studied in experimental osteoarthritis, in patients with mild active systemic lupus erythematosus and in systemic sclerosis patients. In January 2014, the US FDA granted orphan drug designation to paquinimod for the treatment of systemic scleroderma. The Orphan designation is implemented to promote the development of drugs that may provide significant benefit to patients suffering from rare diseases identified as life threatening or chronically debilitating. The further development of paquinimod for systemic lupus erythematosus and rheumatoid arthritis was discontinued.
Status:
Investigational
Source:
NCT02209324: Phase 3 Interventional Completed Herpes Simplex
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Amenamevir is an antiviral agent discovered by Astellas Pharma Inc. and is considered to exert anantiviral effect by inhibiting the activity of the helicase-primase complex, which is involved in DNA replication of herpes virus. It is a helicase-primase inhibitor against herpes simplex virus 1 (HSV-1), HSV-2, and varicella zoster virus. Amenamevir inhibited the in vitro replication of HSV-1 with a mean 50% effective concentration (EC(50)) of 14 ng/ml. Amenamevir was approved in Japan for the treatment of Herpes zoster.
Status:
Investigational
Source:
NCT02251210: Phase 2 Interventional Completed Arthritis, Rheumatoid
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Amelubant, its metabolite BIIL 260 (formed by removal of the ethoxycarbonyl protecting group), and its major metabolite BIIL 315 (formed by removal of the protecting group and glucuronidation) had potent in vitro and in vivo Leukotriene B4 receptor antagonistic properties. Amelubant has been in phase II clinical trials by Boehringer Ingelheim for the treatment of cystic fibrosis, chronic obstructive pulmonay disease, bronchial asthma and rheumatoid arthritis. However, this research has been discontinued. In 2002, orphan drug designation was received in E.U. for the treatment of cystic fibrosis. Serious adverse events of Amelubant were characterized by increased presentation of respiratory signs and/or symptoms associated with pulmonary exacerbation and resulted in admission to a hospital and/or administration of IV antibiotics.
Status:
Investigational
Source:
INN:dexnafenodone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dexnafenodone is a dual of adrenergic receptor antagonist and serotonin uptake inhibitor potentially for the treatment of major depressive disorder. Drug induced a rapid and marked suppression of REM sleep, and in parallel an increase in chin muscle tone during NREM sleep. Dexnafenodone produced a frequency- and voltage-dependent inhibition of the fast sodium channels similar to that exhibited with imipramine. It inhibited voltage- and agonist-stimulated Ca2+ entry in isolated rat aortas. In addition, it decreased Ca2+ content in both resting and noradrenaline-stimulated muscles, suggesting that it may deplete noradrenaline-sensitive intracellular Ca2+ stores. As a consequence, dexnafenodone would reduce the concentration of intracellular free Ca2+ available at the contractile apparatus for vascular smooth muscle contraction. Dexnafenodone exerted fewer cardiodepressant effects than imipramine and desipramine in isolated guinea-pig atrial and ventricular muscle fibres less.
Status:
Investigational
Source:
USAN:Anidoxime
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Anidoxime is unrelated to other analgesic agents in clinical use. It is the hydrochloride salt of 0-(4-methoxyphenyl-carboxyl)-3-diethylamino-propiophenone oxime, with an empirical formula C21H27N3O3 HCl. It was in clinical trial as an oral analgesic agent.