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

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


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.

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

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anilides / chemical synthesis*
  • Anilides / therapeutic use
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical / methods*
  • Cyclohexanes / chemical synthesis*
  • Cyclohexanes / therapeutic use
  • Disease Models, Animal*
  • Humans
  • Injections, Intralesional
  • Male
  • Mice
  • Mice, SCID
  • Pharmaceutical Solutions / chemical synthesis
  • Pharmaceutical Solutions / therapeutic use
  • Prostatic Neoplasms, Castration-Resistant / drug therapy*
  • Rats
  • Treatment Outcome
  • Xenograft Model Antitumor Assays / methods


  • Anilides
  • Antineoplastic Agents
  • Cyclohexanes
  • N-(2,3-dichlorophenyl)cyclohexanecarboxamide
  • Pharmaceutical Solutions