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Updated: Apr 21, 2026
A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Solution formulation development and efficacy of MJC13 in a preclinical model of castration-resistant prostate cancer
Su Liang1, Xiaomei Bian1, Dong Liang1
1a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , Texas Southern University , Houston , TX , USA .
Abstract:
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.
Insights
A new drug, MJC13, effectively reduced castration-resistant prostate cancer tumors in mice. This FKBP52 targeting agent was formulated for improved delivery and showed significant efficacy in preclinical models.
Area of Science:
- Pharmacology
- Oncology
- Drug Development
Background:
- Castration-resistant prostate cancer (CRPC) remains a significant therapeutic challenge.
- FKBP52 is implicated in CRPC progression, making it a viable drug target.
- MJC13 is a novel agent targeting FKBP52 with potential for CRPC treatment.
Purpose of the Study:
- To develop a stable and effective solution formulation for MJC13.
- To evaluate the preclinical efficacy of MJC13 in a CRPC mouse model.
Main Methods:
- Preformulation studies assessed MJC13's physicochemical properties, including lipophilicity and solubility.
- Co-solvent systems were screened to optimize aqueous solubility and formulation tolerance.
- A human prostate cancer xenograft model (22Rv1 cells in SCID mice) was established for efficacy testing.
Main Results:
- MJC13 exhibited poor aqueous solubility (0.28 µg/mL) and high lipophilicity (logP = 6.49).
- An optimal formulation using PEG 400 and Tween 80 (1:1, v/v) achieved a 7.5 mg/mL MJC13 concentration.
- Intratumoral administration of MJC13 (10 mg/kg) twice weekly for four weeks significantly reduced tumor volume in the xenograft model.
Conclusions:
- A stable and effective MJC13 formulation was successfully developed.
- MJC13 demonstrates significant preclinical efficacy against castration-resistant prostate cancer in a xenograft model.
- MJC13 represents a promising therapeutic candidate for CRPC treatment.
