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

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Showing 541 - 550 of 4710 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)



Icomucret (15(S)-HETE) is an hydroxyeicosatetraenoic acid developed by Alcon Research, Ltd for treatment Ophthalmic Disorders. In vitro Icomucret has been shown to inhibit LTB4 formation, 12-HETE formation and specifically inhibits the neutrophil chemotactic effect of LTB4. The inhibition of LTB4 formation is probably due to modulation of the 5- lipoxygenase (LO) because no changes in PGE2 formation have been determined. In vivo, Icomucret inhibits LTB4-induced erythema and edema, and reduces LTB4 in the synovial fluid of carragheenan-induced experimental arthritis in dogs. Icomucret has also some immunomodulatory effects. It inhibits the mixed lymphocyte reaction, induces generation of murine cytotoxic suppressor T cells, and it decreases interferon production by murine lymphoma cells. Furthermore, IL-4 and IL-13 have recently been shown to be potent activators of the 15-LO in mononuclear cells. Icomucret induces the secretion of membrane-bound mucins from human conjunctival and corneal epithelial cells. Icomucret was evaluated in clinical trials for Dry Eye Syndrome treatment. However from 2007 no future development reported, and Icomucret development sims to be discontinued.
Status:
Investigational
Source:
Tokai J Exp Clin Med. May 1990;15(2-3):123-7.: Not Applicable Human clinical trial Completed Liver Cirrhosis, Alcoholic/physiopathology
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00000806: Phase 1 Interventional Completed HIV Infections
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Telinavir (previously known as SC-52151) was developed as an anti-HIV aspartyl protease inhibitor for the treatment of HIV Infections. Telinavir participated in Phase I/II clinical study. In spite of the drug was well tolerated no antiviral activity was produced and further development of the drug was discontinued.
Status:
Investigational
Source:
USAN:CYPOTHRIN [USAN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Cypothrin is a synthetic pyrethroid insecticide, developed by American Cyanamide for the control of ticks and marketed under the tradename Panecto. The compound exhibited systemic insecticidal activity in the model of flies infestation in mice and ixodicidal activity in against larvae of Boophilus microplus.
Status:
Investigational
Source:
INN:dagapamil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dagapamil is a calcium-channel blocker, discovered by BASF. The compound is claimed to have antihypertensive, antiarrhythmic, cardioprotective, antiallergic and platelet aggregation-inhibiting action in animal models.
Status:
Investigational
Source:
INN:levomequitazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levomequitazine is the L-enantiomer of mequitazine. The antihistaminergic activity mainly resides in the S-enantiomer, L-mequitazine, whereas the anticholinergic activity mainly resides in the D-enantiomer. It was shown, that L-enantiomer of mequitazine is less potent antagonist of human M3 muscarinic acetylcholine receptors than D-enantiomer. In vitro binding studies have shown that the affinity of L-mequitazine for H1 receptors is approximately ten times higher and to muscarinic receptors ten times lower, compared to d-mequitazine. Memory impairment was observed after administration of L-mequitazine 10 mg alone on delayed recall. This could be due to indirect effects of H1 receptor blockade. L-mequitazine 10 mg produced mild driving impairment, whereas L-mequitazine 2.5 and 5.0 mg show no effects on driving. Levomequitazine had been in phase III clinical trials by Pierre Fabre for the treatment of perennial allergic rhinitis and seasonal allergic rhinitis.
Status:
Investigational
Source:
INN:nicotredole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nicotredole (Tryptamide), similarly to ibuprofen and piroxicam, shows anti-inflammatory and analgesic properties. Tryptamide reversed pyrogen-induced hyperthermia in rats, elicited analgesic effects in rats, but not in mice, prolonged the time of hexobarbital sleep in rats and inhibited locomotor activity in rats and mice. Tryptamide has not elicited side effects on the circulatory system of rats and cats.
Status:
Investigational
Source:
INN:lobuprofen [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lobuprofen is an ester type analgesic, in which the acid moiety (ibuprofen) has peripheral analgesic activity and the alcohol moiety (mCPPol) has central analgesic activity.
Status:
Investigational
Source:
NCT01362400: Phase 2 Interventional Completed Non Small Cell Lung Cancer
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Retaspimycin (IPI-504) was previously under development by manufacturer Infinity Pharmaceuticals in conjunction with MedImmune, a part of AstraZeneca. Retaspimycin is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. Orphan drug designation was assigned to the compound by the FDA for the treatment of gastrointestinal stromal cancer (GIST). Infinity Pharmaceuticals has discontinued the development of retaspimycin (IPI-504) an inhibitor of the HSP-90) complex, for the treatment of cancer due to lack of efficacy in 1913.
Status:
Investigational
Source:
INN:cefsumide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefsumide is an antibiotic of the cephalosporin group patented by Fujisawa Pharmaceutical Co. Cefsumide binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.