New, oral LHRH antagonists in treatment of prostate cancer?


At least three new LHRH receptor antagonists — i.e., drugs similar to degarelix (Firmagon) — are in development at the present time: elagolix, relugolix, and ASP-1707. However, unlike degarelix, all three are agents that would act as oral drugs as opposed to drugs one has to be given as long-term injections.

At present, these drugs are also all in initial development for the treatment of endometriosis in women, and not for treatment of prostate cancer … but then that’s what originally happened with the early development of drugs like leuprolide actetate (Lupron) and the other LHRH agonists back in the 1980s too.

Do new, oral LHRH receptor antagonists have potential in the management of prostate cancer? Sure they do … if they have similar effectiveness to the available, injectable agents; if they can lower the risk for short- and long-term side effects; and if they are affordable for patients. Of course those are three pretty big “ifs”.

The drug that seems to be in the most advanced stages of development is elagolix, which is currently being tested in a randomized, global, Phase III clinical trial for the treatment of endometriosis. ASP-1707 is being tested for treatment of endometriosis in a 600-patient Phase II trial. Relugolix (also known as TAK-385) is being evaluated in a similarly large Phase II study.

At the moment we have seen only one sign of a trial in prostate cancer (a possible Phase I trial of ASP-1707 in Europe) … but the drugs’ developers are, clearly, well aware of this opportunity.

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