Delving into the Latest Updates on B-4112 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Mechanism-

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

University of Pretoria

Active Organization-

Inactive Organization

University of Pretoria

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

The multidrug resistance (MDR)-neutralizing and cytotoxic properties of five tetramethylpiperidine (TMP)-substituted phenazines were compared with those of their corresponding isopropyl-substituted analogues using a P-glycoprotein (P-gp)-expressing small cell lung cancer cell line (H69/LX4). All of the TMP-substituted phenazines tested outperformed their isopropyl analogues with respect to both cytotoxic and chemosensitizing properties, indicating the importance of TMP-substitution when designing novel riminophenazines with increased activity against MDR cancer cell lines. Of the TMP-substituted phenazines tested, B4112, chlorinated at position 3 of the phenyl- and anilino-rings, had the most potent anti-cancer activity in vitro, making this agent a potential candidate for evaluation in experimental and clinical oncology.

01 Dec 1999·Annals of the New York Academy of SciencesQ2 · CROSS-FIELD

B4112, a Novel Tetramethylpiperidine‐Substituted Phenazine That Inhibits the Proliferation of Multidrug‐Resistant Cancer Cell Lines

Q2 · CROSS-FIELD

Review

Author: R. Anderson ; G. Jooné ; E. Niekerk ; C.E. J. Rensburg

The efficacy of B4112 against multidrug resistant cancer cell lines was examined in vitro.The effects of B4112 (0.01-1 μg/mL) alone and in the presence of vinblastine (3 ng/mL) were examined on the proliferation of a P-glycoprotein-expressing erythroleukemic cell line.At 8 ng/mL, B4112 caused 50% restoration of chemosensitivity of this cancer cell line to vinblastine, while the corresponding concentration of B4112, which caused 50% direct cytotoxicity, was 200 ng/mL.B4112 inhibited growth of colon, liver, esophageal, and prostate cancer cell lines with varying patterns of intrinsic multidrug resistance by 50% at 0.29-0.98 μg/mL after exposure for 3-4 days.

100 Deals associated with B-4112

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