TREATMENT METHODS USING PHARMACEUTICAL SOLID STATE FORMS
The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions.
1 . A method to treat a cancer or precancer in a subject in need thereof, comprising administering to the subject or delivering to the subject's tissues an effective amount of crystalline 17α-ethynyl-5α-androstane-3α,17β-diol, or a formulation comprising or consisting of crystalline 17α-ethynyl-5α-androstane-3α,17β-diol and at least one excipient or one or more excipients, or a formulation prepared from crystalline 17α-ethynyl-5α-androstane-3α,17β-diol and one, two, three, four or more excipients.
2 . The method of claim 1 wherein the cancer is prostate cancer, breast cancer, ovarian cancer, cervical cancer, endometrial cancer or benign prostatic hypertrophy.
3 . The method of claim 1 wherein the crystalline 17α-ethynyl-5α-androstane-3α,17β-diol is a crystalline anhydrate.
4 . The method of claim 3 wherein the crystalline anhydrate 17α-ethynyl-5α-androstane-3α,17β-diol is Form III.
5 . The method of claim 1 wherein the precancer is prostatic interstitial neoplasia, cervical dysplasia or ductal carcinoma in situ.
6 . The method of claim 1 further comprising administering to the subject or delivering to the subject's tissues an effective amount of an anti-microtubule agent, or administering to the subject or delivering to the subject's tissues a formulation further comprising an anti-microtubule agent, or a formulation consisting of crystalline 17α-ethynyl-5α-androstane-3α,17β-diol, an anti-microtubule agent and one or more excipients, or a formulation prepared from crystalline 17α-ethynyl-5α-androstane-3α,17β-diol, an anti-microtubule agent and one, two, three, four or more excipients.
7 . The method of claim 6 wherein the anti-microtubule agent is a taxane compound.
8 . The method of claim 6 wherein the anti-microtubule agent is paclitaxel or docetaxel.