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Pharm Dev Technol. 2016;21(1):121-6. doi: 10.3109/10837450.2014.979946. Epub 2014 Nov 7.

Solution formulation development and efficacy of MJC13 in a preclinical model of castration-resistant prostate cancer.

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a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , Texas Southern University , Houston , TX , USA .
b Department of Biological Sciences, Border Biomedical Research Center , University of Texas at El Paso , El Paso , TX , USA , and.
c Urologic Oncology Branch , National Cancer Institute , Bethesda , MD , USA.


MJC13, a novel FKBP52 targeting agent, has potential use for the treatment of castration-resistant prostate cancer. The purpose of this work was to develop a solution formulation of MJC13, and obtain its efficacy profile in a human prostate cancer xenograft mouse model. Preformulation studies were conducted to evaluate the physicochemical properties. Co-solvent systems were evaluated for aqueous solubility and tolerance. A human prostate cancer xenograft mouse model was established by growing 22Rv1 prostate cancer cells in C.B-17 SCID mice. The optimal formulation was used to study the efficacy of MJC13 in this preclinical model of castrate-resistant prostate cancer. We found that MJC13 was stable (at least for 1 month), highly lipophilic (logP = 6.49), poorly soluble in water (0.28 µg/mL), and highly plasma protein bound (>98%). The optimal formulation consisting of PEG 400 and Tween 80 (1:1, v/v) allowed us to achieve a MJC13 concentration of 7.5 mg/mL, and tolerated an aqueous environment. After twice weekly intratumoral injection with 10 mg/kg MJC13 in this formulation for four consecutive weeks, tumor volumes were significantly reduced compared to vehicle-treated controls.


Androgen-independent; MJC13; castration-resistant prostate cancer; efficacy; formulation; preformulation

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