Delving into the Latest Updates on 1954U89 with Synapse

Overview

Basic Info

Drug Type

Unknown

Synonyms

Target-

Mechanism-

Therapeutic Areas

NeoplasmsInfectious DiseasesRespiratory Diseases+ [1]

Active Indication-

Inactive Indication

CandidiasisNeoplasmsPneumonia, Pneumocystis

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK Plc

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

1954U89, 1,3-diamino-7-(1-ethylpropyl)-8-methyl-7H-pyrrolo-(3, 2-f)quinazoline, is a potent, lipid-soluble inhibitor of dihydrofolate reductase. The pharmacokinetics and bioavailability of 1954U89 were examined in male beagle dogs and male CD rats. Dogs received single intravenous (2.5 mg kg-1) and oral (5.0 mg kg-1) doses of 1954U89 with and without successive administration of calcium leucovorin. Single intravenous (5.0 mg kg-1) and oral (10 mg kg-1) doses of [1,3-14C2]1954U89 were administered to rats. Plasma concentrations of total radiocarbon were determined by scintillation counting, and intact 1954U89 was measured by HPLC. The mean plasma half-life was 3.2 +/- 0.62 and 4.2 +/- 0.68 h after intravenous and oral administration, respectively, to dogs. The pooled plasma half-life after intravenous administration to rats averaged 1.2 h; a reliable plasma half-life value after oral administration could not be determined. Mean total-body clearance was 2.4 +/- 0.39 and 4.5 +/- 1.1 L h-1 kg-1 after intravenous and oral administration, respectively, to dogs, and averaged 12 and 77 L h-1 kg-1 after intravenous and oral administration, respectively, to rats. Neither clearance nor bioavailability of 1954U89 in dogs was affected significantly by administration of calcium leucovorin. Absolute bioavailability was 54 +/- 12% in dogs and 16% in rats.

100 Deals associated with 1954U89

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Candidiasis	Preclinical	US	GSK Plc	-
Candidiasis	Preclinical	GB	GSK Plc	-
Neoplasms	Preclinical	US	GSK Plc	-
Neoplasms	Preclinical	GB	GSK Plc	-
Pneumonia, Pneumocystis	Preclinical	GB	GSK Plc	-
Pneumonia, Pneumocystis	Preclinical	US	GSK Plc	-