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

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Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.
Status:
Investigational
Source:
INN:doqualast
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Doqualast is an antiasthmatic and antiallergic agent. It has a mode of antiallergic action similar to that of disodium cromoglycate and inhibits antigen-induced mediator release by interfering with the calcium transport required for histamine secretion across the mast cell membrane. In rabbits, no embryotoxic or teratogenic effects of doqualast were observed. The concomitant use of doqualast and theophylline might cause drug interaction. Doqualast is thought to increase the blood free fraction of concomitantly used theophylline and to accelerate elimination of theophylline from blood.
Status:
Investigational
Source:
INN:tianafac
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Tianafac (also known as L8109) is a thienylacetic acid derivative patented by Labaz group as antipyretics and anti-inflammatory agent useful for the treatment of arthritis. In preclinical models, Tianafac inhibits prostaglandin formation by seminal vesicle microsomes and exerts antipyretic, analgetic, and moderate gastric ulcerogenic activity and had a wide safety margin between toxic and pharmacologically active doses.
Status:
Investigational
Source:
INN:pipoxizine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pipoxizine is the antihistamine agent and antiserotonin agent. It was used as antiarrhythmic and bronchodilator.
Status:
Investigational
Source:
INN:menitrazepam
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Menitrazepam is a cyclohexene-substituted benzodiazepine. It is a muscle relaxant.
Status:
Investigational
Source:
INN:balamapimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Balamapimod, also known as MKI 833, a mitogen-activated protein kinase (Ras/Raf/MEK) inhibitor with potential anti-tumor activity. This compound can be used for the treatment of diseases that are results of deregulation of Ras/Raf/MEK kinases.
Status:
Investigational
Source:
INN:nonabine
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Nonabine is a chromenol structurally related to the cannabinoids which has shown antiemetic efficacy in clinical trials. Nonabine also produced sedative clinical effects, but with an EEG profile which resembled that reportedly caused by cannabinoids. In contrast to cannabinoids, nonabine did not cause changes of mood or perception, suggesting that nonabine lacks the potential for social abuse at antiemetic doses. Nonabine was studied in the 1980s for the prevention of nausea and vomiting associated with cancer chemotherapy.
Status:
Investigational
Source:
INN:indocate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Indocate is indole derivative and monoamine oxidase inhibitor with peripheral antiserotonin properties.
Status:
Investigational
Source:
INN:etazepine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Etazepine (5,6-dihydro-5-methyl-11H-11-ethoxy-dibenzo[b,e]azepin-6-one) demonstrates anticonvulsant activity in rodents. Etazepine seems to exert its anticonvulsant effects by activating the GABAergic system.
Status:
Investigational
Source:
INN:taltrimide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Taltrimide, a taurine derivative that was developed as an anticonvulsive agent. Taltrimide strongly inhibits the sodium-independent binding of taurine to synaptic membranes of the brain and it does not appear to bind to GABAA and benzodiazepine receptor. The drug was studied in phase II clinical trial Finland as an anticonvulsant agent to treat epilepsy. However, the further development of this drug was discontinued.