Drug intelligence / Profile preview

PK11195

Development stage
Phase 4
Modality
Small Molecules
Administration
Intravenous
01

Overview

PK11195 is a synthetic small molecule that acts as a selective antagonist of the translocator protein (TSPO), formerly known as the peripheral benzodiazepine receptor (PBR). It binds with high affinity to TSPO and has been widely used as a research tool and radioligand marker for imaging neuroinflammation and neuronal damage in animal models and humans. The compound is also studied for its ability to induce apoptosis in certain cancer cells (notably chronic lymphocytic leukemia) by mechanisms involving mitochondrial depolarization and cytochrome c release. In addition to its use in positron emission tomography (PET) imaging—especially when radiolabeled ([11C]PK11195)—it has been investigated preclinically for potential anticancer effects and chemosensitization of tumor cells but has not advanced beyond early-stage research[4][5][7][8][9].

Other names
1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamideN-sec-Butyl-1-(2-chlorophenyl)-N-methyl-3-isoquinolinecarboxamideUNII-YNF83VN1RLUNII-YNF-83VN1RLUNII-YNF 83VN1RL
02

Targets

MPTP (Mitochondrial permeability transition pore)ABCB1 (P-glycoprotein)TSPO (Translocator Protein (18 kDa))

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