Elesclomol

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Synonym(s)

STA 4783

Definition
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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)
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  • 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 use
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Still in the experimental stage.

Note(s)
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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.

Literature
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  1. Hauschild A et al (2008) systemic therapy of melanoma. Current clinical studies. dermatologist 59: 484-492

Incoming links (2)

Heat-shock proteins; Paclitaxel;

Authors

Last updated on: 29.10.2020