Investigational developments for the treatment of progesterone-dependent diseases

Möller C, Carsten Möller, Jens Hoffmann, Kirkland TA, Thomas A. Kirkland, Wolfgang Schwede, Schwede W
Expert opinion on investigational drugs · 2008 · vol. 17(4) , pp. 469–479 · doi:10.1517/13543784.17.4.469 · PMID:18363513 · W2159309145
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This review examines the development of progesterone receptor antagonists and modulators for treating uterine fibroids, endometriosis, and breast cancer, highlighting their effectiveness and future potential.

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Abstract

BACKGROUND: Clinical evidence has shown that conditions such as uterine fibroids, endometriosis and breast cancer are progesterone-dependent diseases. Therefore, progesterone receptor (PR) antagonists and selective PR modulators (SPRMs) are under development for the treatment of these conditions. However, the first PR antagonists that became available exhibit insufficient selectivity or tolerability for the chronic administration required to treat these conditions. Despite initial setbacks, development of second-generation PR antagonists with better selectivity continues forward. OBJECTIVE: In this review we would like to summarise prospects for using PR antagonists for the treatment of uterine fibroids, endometriosis and breast cancer, and to give an overview of the development of new steroidal and non-steroidal PR antagonists. METHOD: Available preclinical and clinical data and publications have been reviewed with the focus on scientific background and use in the three mentioned indications. RESULTS/CONCLUSION: Preclinical and clinical evidence demonstrated that PR antagonists and SPRMs are effective for the treatment of progesterone-dependent diseases. Future development will demonstrate if they can become important drugs.

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Condition tags

endometriosis

MeSH descriptors

Antineoplastic Agents Drugs, Investigational Hormone Antagonists Progesterone Receptors, Progesterone Animals Animals Antineoplastic Agents Antineoplastic Agents Antineoplastic Agents Breast Neoplasms Breast Neoplasms Breast Neoplasms Breast Neoplasms Cell Proliferation Cell Proliferation Cell Proliferation Drug Partial Agonism Drug Partial Agonism Drugs, Investigational

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