On June 6, 2013 Isis Pharmaceuticals reported that it has earned a $6 million payment from AstraZeneca related to continuation of the research collaboration between Isis and AstraZeneca to discover and develop novel antisense therapeutics to treat cancer (Press release Isis Pharmaceuticals, JUN 6, 2013, View Source;p=irol-newsArticle&ID=1827576&highlight= [SID:1234500201]). In addition to the research collaboration, which includes three cancer targets, Isis and AstraZeneca are developing two antisense drugs, ISIS-ARRx and ISIS-STAT3Rx, discovered by Isis and licensed to AstraZeneca for the treatment of cancer.

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Does the novel progesterone receptor (PR) modulator BAY 1002670, based on its preclinical pharmacological profile, offer a potential novel treatment option for uterine fibroids?
The newly synthesized BAY1002670 has proved to be a very potent, highly selective PR modulator in all in vitro and in vivo pharmacodynamics assays performed: it exhibits marked efficacy in an innovative humanized fibroid disease model, suggesting BAY 1002670 to be a very promising treatment option for uterine fibroids.
PR inhibiting ligands have shown clinical utility in a range of potential indications and applications. Despite the emergence of the first PR antagonist >30 years ago, no agent of this compound class has been authorized in any indication for long-term application. Among other reasons, suboptimal selectivity and safety profiles of previous candidates have led to discontinuation and modification of development programmes.
The preclinical studies include relevant in vitro and in vivo assays to clarify the properties of the PR modulator BAY 1002670 as well as a fibroid xenograft study to show directly the efficacy of BAY 1002670 on the human target tissue.
BAY 1002670 was tested for binding and transactivational activity towards different human steroid receptors. Activity of the compound in the corresponding in vivo models (rat, rabbit) was assessed. Furthermore, BAY 1002670 was tested in a disease model for uterine fibroids utilizing primary human tumour tissues as xenograft in immunodeficient mice treated with estradiol (E2) and progesterone (P).
BAY1002670 in subnanomolar concentrations exhibits a highly selective binding profile and antagonistic activity for the PR. These properties are also reflected in its action in two progesterone-dependent animal models that assess the termination of pregnancy and endometrial transformation. Favourable selectivity towards other nuclear hormone receptors was demonstrated. No in vivo activity was found at the glucocorticoid, estrogenic and mineralocorticoid receptors with only weak anti-androgenic activity. In a human fibroid xenograft model BAY 1002670 showed a marked dose-dependent reduction of fibroid tumour weight gain of 95% at a dose of 3 mg/kg/day (P < 0.005).
Selectivity and potency of BAY 1002670 have only been determined in vitro and in animal models so far.
The PR modulator BAY 1002670 might offer a treatment option not only for uterine fibroids but also for other gynaecological indications.
The studies took place at Bayer Pharma AG. All authors are employees of Bayer Pharma AG. No external funding declared.

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(Press release, EGEN Inc, JUN 5, 2013, View Source;advances-a-systemically-delivered-rnai-therapeutic-for-the-treatment-of-pulmonary-arterial-hypertension-pah-210247491.html [SID:1234504979])

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(Press release, Inflection Biosciences, JUN 4, 2013, View Source [SID:1234503414])

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On March 6, 2013 Vernalis plc and Servier, France’s largest privately-owned pharmaceutical company, reported the further extension of their ongoing oncology collaboration initiated in May 2007 (Press release, Servier, JUN 3, 2013, View Source [SID:1234508823]).

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This is the first of three collaborations between Vernalis and Servier and focuses on multiple undisclosed oncology targets. It was initially extended in October 2011 and is now extended for a further two years.

Ian Garland, CEO of Vernalis, commented "We are delighted by this news which reflects Servier’s continued endorsement of our joint achievements over the past few years."

Servier’s head of research, Bernard Marchand, said: "this 2-year extension highlights our commitment to cancer research through innovative drug discovery platforms."