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

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Showing 11 - 18 of 18 results

Status:
Investigational
Source:
INN:ormaplatin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Targets:

Conditions:

Ormaplatin (NSC 363812, tetraplatin) is a stable platinum (IV) analog. Ormaplatin alkylates DNA, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. Ormaplatin showed marked antitumor activity both in vitro and vivo. The severe, cumulative and irreversible peripheral neurotoxicity observed in phase I studies resulted in termination of further clinical development of ormaplatin.
Status:
Investigational
Source:
INN:ormaplatin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Ormaplatin (NSC 363812, tetraplatin) is a stable platinum (IV) analog. Ormaplatin alkylates DNA, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. Ormaplatin showed marked antitumor activity both in vitro and vivo. The severe, cumulative and irreversible peripheral neurotoxicity observed in phase I studies resulted in termination of further clinical development of ormaplatin.
Status:
Investigational
Source:
INN:sonepiprazole
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Sonepiprazole exhibits highly specific binding to the D4 dopamine receptor with more than 100-fold selectivity for the D4 receptor over other receptors, including dopamine, serotonin, and adrenergic receptors. It is a neutral antagonist at the D4 dopamine receptor and is devoid of dopamine agonist activity. Sonepiprazole selectively induces c-fos expression in the prefrontal cortex and blocks behavioral, biochemical, and genomic effects of repeated amphetamine administration in rats. Sonepiprazole was investigated as an antipsychotic for the treatment of schizophrenia in a placebo-controlled clinical trial, but in contrast to its comparator olanzapine no benefits were found and it was not researched further for this indication.
Status:
Investigational
Source:
INN:piriprost
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Piriprost (U-60, 257) is a structural analog of prostaglandin I2 (PGI2) with low IP receptor-mediated activity. It inhibits 5-LO (5-lipoxygenase). Piriprost inhibits the release of histamine and leukotrienes, implicating its role in inflammation and allergic responses. However, it was shown, that piriprost did not influence the airway responses after allergen in asthma. Nevertheless, even more, the drug was irritant to the respiratory tract than was placebo.
Ritipenem (FCE 22101), a penem antibiotic, penicillin binding protein inhibitor, is potent against both gram-positive and -negative bacteria, and its acetoxymethyl ester (FCE 22891; ritipenem-acoxil) is orally available. Ritipenem is manufactured by Tanabe Seiyaku in the ritipenem acoxil prodrug form, which can be taken orally. It is not FDA approved in the United States.
Ritipenem (FCE 22101), a penem antibiotic, penicillin binding protein inhibitor, is potent against both gram-positive and -negative bacteria, and its acetoxymethyl ester (FCE 22891; ritipenem-acoxil) is orally available. Ritipenem is manufactured by Tanabe Seiyaku in the ritipenem acoxil prodrug form, which can be taken orally. It is not FDA approved in the United States.
Ritipenem (FCE 22101), a penem antibiotic, penicillin binding protein inhibitor, is potent against both gram-positive and -negative bacteria, and its acetoxymethyl ester (FCE 22891; ritipenem-acoxil) is orally available. Ritipenem is manufactured by Tanabe Seiyaku in the ritipenem acoxil prodrug form, which can be taken orally. It is not FDA approved in the United States.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Amperozide (FG 5606, N-ethyl-4-[4',4'-bis(p-fluorophenyl)butyl]-1-piperazine-carboxamide) is an atypical antipsychotic drug which has relatively weak in vitro affinity for striatal dopamine2 (D2) receptors and a strong affinity for the cortical 5-HT2A receptor. It was shown in animal models, that amperozide could attenuate craving for cocaine. In addition, this drug was studied in patients with schizophrenia and was shown, that several patients had improvements as was assessed by the Clinical Global Improvement Scale. However, these studies were discontinued.

Showing 11 - 18 of 18 results