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Showing 961 - 970 of 34955 results

Status:
Investigational
Source:
JAN:FERROUS OROTATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

There is no information about biological o medical application of ferrous orotate. But is known, that this substance may be used for nutritional purposes to food supplements.
Status:
Investigational
Source:
NCT04669067: Phase 1/Phase 2 Interventional Active, not recruiting Acute Myeloid Leukemia
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is currently in clinical trials. Based on X-ray cocrystal structures a model of AMG 232 bound to MDM2 was developed. The model shows that the m-chlorophenyl, the p-chlorophenyl, and C-linked isopropyl fragments of AMG 232 bind to the Leu 26(p53), Trp 23(p53), and Phe 19(p53) pockets of MDM2, respectively. The carboxylic acid forms a salt bridge with His 96 and the isopropyl sulfone forms a novel interaction with the glycine shelf region of MDM2. AMG 232 in phase II in combination with trametinib and dabrafenib in subjects with metastatic melanoma; in phase I for the treatment of solid tumors, multiple myeloma and Acute Myeloid Leukemia.
Status:
Investigational
Source:
NCT03078322: Phase 2 Interventional Completed Major Depressive Disorder
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

4‐Chlorokynurenine (AV-101) is a neuropharmaceutical drug candidate in development for the treatment of major depressive disorder. Pharmacology studies conducted in rodent models have demonstrated AV-101’s antihyperalgesic activity in models of facilitated pain processing was seen at serum concentrations ranging from 150–300 M. In addition, AV-101 has been shown to be neuroprotective activity against an intrahippocampal injection of quinolinic acid, reductions in seizures, and antidepressive activity. An oral prodrug, AV-101, which, in the brain, is converted into one of the most potent and selective GlyB site antagonists of the NMDAR, has been demonstrated to be active in animal models of neuropathic pain. The two Phase 1 studies were designed to assess the safety and pharmacokinetics of AV-101, over a wide dose range, after daily dosing for 14-days. AV-101 has excellent safety and PK characteristics providing support for advancing AV-101 into Phase 2 studies in neuropathic pain.
Status:
Investigational
Source:
NCT02113163: Phase 1 Interventional Completed Diabetes Mellitus, Non-Insulin-Dependent
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02435199: Phase 2 Interventional Withdrawn Diabetic Neuropathies
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Olodanrigan (EMA-401) is an angiotensin II type 2 receptor antagonist. Olodanrigan may act on paracrine/autocrine mechanisms at peripheral nerve terminals, or intracrine mechanisms, to reduce neuropathic pain signalling in AngII/NGF/TRPV1-convergent pathways. Olodanrigan is being developed by Novartis for the treatment of neuropathic pain.
Status:
Investigational
Source:
NCT01832298: Phase 1 Interventional Completed Advanced Solid Tumor
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

HaiHe Biopharma (Shanghai HaiHe Pharmaceutical) is developing simmitecan, an ester pro-drug of chimmitecan for the treatment of cancer. Simmitecan is in phase I development for solid tumours and colorectal cancer in China. Simmitecan (L-P) is a water-soluble ester prodrug of chimmitecan (L-2-Z) with potent anti-tumor activities in different experimental animals. Chimmitecan,a novel CPT derivative, exhibited potent antitumor activities both in vitro and in vivo by inhibiting topoisomerase I.
Status:
Investigational
Source:
NCT04327024: Phase 2 Interventional Completed Heart Failure With Preserved Ejection Fraction (HFpEF)
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Verinurad (RDEA3170) is a selective uric acid reabsorption inhibitor in clinical development for the treatment of gout and asymptomatic hyperuricemia. Verinurad specifically inhibits URAT1 with a potency of 25 nM. High affinity inhibition of uric acid transport requires URAT1 residues Cys-32, Ser-35, Phe-365 and Ile-481. Unlike other available uricosuric agents, the requirement for Cys-32 is unique to verinurad. Verinurad doses as low as 2.5 mg produce significant sUA lowering in humans, and this greater reduction in sUA may lead to improved outcomes and medical benefits for patients with gout. Verinurad in monotherapy studies has been associated with increased urinary uric acid concentrations and low rates of serum creatinine (sCr) elevation. Verinurad combined with febuxostat decreased sUA dose-dependently while maintaining uric acid excretion similar to baseline. All dose combinations of verinurad and febuxostat were generally well tolerated.
Status:
Investigational
Source:
INN:nobiprostolan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mallinckrodt (previously Sucampo Pharmaceuticals) is developing nobiprostolan (RK 023), a topical therapy for male pattern baldness (androgenetic alopecia) and hypotrichosis. The drug is a physiologically active fatty acid derivative. Nobiprostolan is in Phase IIa clinical trials for the treatment of male pattern baldness.
Status:
Investigational
Source:
NCT02255812: Not Applicable Interventional Completed Exploratory Behavior
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00972322: Phase 1 Interventional Completed Type 2 Diabetes Mellitus
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Merck was developing MK 8245, an orally active inhibitor of stearoyl CoA desaturase for the treatment of type-2 diabetes mellitus. MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. It is in Phase 2 clinical studies for type 2 diabetes mellitus.