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

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Showing 451 - 460 of 13408 results

Status:
Investigational
Source:
INN:adaprolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.
Status:
Investigational
Source:
INN:diamfenetide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Diamfenetide (aka diamphenethide) is a fasiolicide used in sheep. It is effective against immature flukes but with diminishing activity as the fluke ages. It has proven an effective compound for use in prophylactic programs against Fasciola hepatica. Diamphenethide is deacetylated in the host liver to an active monoamine and diamine. The amine of diamfenetide has an action which produces an elevation of malate concentration in Fasciola. Malate is an intermediary product of glucose in this parasite. It is known that dopamine, a putative neurotransmitter in Fasciola has a protective effect against diamfenetide but the mode of action of a diamfenetide has yet to be defined in greater detail.
Status:
Investigational
Source:
INN:denibulin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Denibulin is a novel antineoplastic agent. Denibulin selectively targets and reversibly binds to the colchicine-binding site on tubulin and inhibits microtubule assembly. This results in the disruption of the cytoskeleton of tumor endothelial cells, ultimately leading to cell cycle arrest, blockage of cell division and apoptosis. This causes inadequate blood flow to the tumor and eventually leads to a decrease in tumor cell proliferation. Denibulin hydrochloride had been in phase I clinical trials for the treatment of solid tumours. It was generally well tolerated and showed decrease in tumor vascular parameters. However, no recent development has been reported.
Status:
Investigational
Source:
INN:milveterol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Milveterol (also known as GSK159797) was developed as a longer-acting beta2 adrenoceptor agonist for the treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). Milveterol completed phase II clinical trials for asthmatic subjects. However further development of the drug was discontinued.
Status:
Investigational
Source:
INN:enestebol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Enestebol is an anabolic steroid.
Status:
Investigational
Source:
INN:metribolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Metribolone, also known as methyltrienolone, an anabolic agent, binds to the androgen receptor and was studied for the treatment of advanced breast cancer. However, because of the liver toxicity, further development of this drug was discontinued. Now, this compound is used for research purpose as synthetic androgen.
Status:
Investigational
Source:
INN:varoglutamstat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Peliglitazar (also known as BMS 426707-01), a dual α/γ peroxisome proliferator-activated receptor agonist, has been studied in phase I/II clinical trial in patients with type 2 diabetes mellitus. However, this study was discontinued.
Ertiprotafib was originally developed as an inhibitor of PTP1B. Multiple targets of ertiprotafib, in addition to PTP1B inhibition, have been suggested including dual PPARalpha/PPARgamma agonism and IKK-beta inhibition. It normalized the plasma glucose and insulin levels in diabetic animal models and progressed to a phase II clinical trial for the treatment of Type 2 diabetes mellitus. Ertiprotafib development has been discontinued.
Status:
Investigational
Source:
INN:cyclobutoic acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Cyclobutoic acid is a synthetic analog of mevalonic acid, developed by the Italian company Farmitalia Carlo Erba SPA. The compound inhibited the incorporation of [14C] into CO2, fatty acids and cholesterol, and was used for the treatment of hepatic deficiency.