Elesclomol
Synonym(s)
STA 4783
DefinitionThis section has been translated automatically.
Inducer of oxidative stress in tumor cells ("small molecule"). Currently orphan drug status(approved by the FDA as an orphan drug for the treatment of malignant melanoma).
Pharmacodynamics (Effect)This section has been translated automatically.
- Elesclomol induces the formation of the heat shock protein 70 (see below heat shock proteins). The resulting oxidative stress causes an increased apoptosis or an increased sensitivity to certain other cytostatic drugs, e.g. paclitaxel.
- The drug induces oxidative stress in tumour cells. This means that increased concentrations of so-called reactive oxygen species(ROS) are present. In contrast to normal cells, degenerated cells typically contain much higher concentrations of ROS. Furthermore, the antioxidative capacity of tumour cells is reduced, so that programmed cell death ( apoptosis) is initiated when the ROS concentration exceeds a critical threshold value.
Dosage and method of useThis section has been translated automatically.
Still in the experimental stage.
Note(s)This section has been translated automatically.
In a randomized, placebo-controlled, double-blind study involving 21 centers, the efficacy of elesclomol was demonstrated in 81 patients with metastatic melanoma. In combination with paclitaxel, the progression-free survival time was doubled compared to paclitaxel monotherapy. Even more significant were the differences in progressive free survival for patients who had not previously received chemotherapy.
LiteratureThis section has been translated automatically.
- Hauschild A et al (2008) systemic therapy of melanoma. Current clinical studies. dermatologist 59: 484-492