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Phase I Study of PSMA-Targeted Docetaxel-Containing Nanoparticle BIND-014 in Patients with Advanced Solid Tumors
Daniel D Von Hoff1, Monica M Mita2, Ramesh K Ramanathan3
1Translational Genomic Research Institute and Virginia G. Piper Cancer Center, Scottsdale, Arizona.
Purpose:
First-in-human phase I trial to determine the safety, pharmacokinetics, and antitumor activity of BIND-014, a novel, tumor prostate-specific membrane antigen (PSMA)-targeted nanoparticle, containing docetaxel.
Experimental Design:
Patients with advanced solid tumors received BIND-014 every three weeks (n = 28) or weekly (n = 27), with dose levels ranging from 3.5 to 75 mg/m(2) and 15 to 45 mg/m(2), respectively.
Results:
BIND-014 was generally well tolerated, with no unexpected toxicities. The most common drug-related toxicities (>20% of patients) on either schedule included neutropenia, fatigue, anemia, alopecia, and diarrhea. BIND-014 demonstrated a dose-linear pharmacokinetic profile, distinct from docetaxel, with prolonged persistence of docetaxel-encapsulated circulating nanoparticles. Of the 52 patients evaluable for response, one had a complete response (cervical cancer on the every three week schedule) and five had partial responses (ampullary adenocarcinoma, non-small cell lung, and prostate cancers on the every-three-week schedule, and breast and gastroesophageal cancers on the weekly schedule). Responses were noted in both PSMA-detectable and -undetectable tumors.
Conclusions:
BIND-014 was generally well tolerated, with predictable and manageable toxicity and a unique pharmacokinetic profile compared with conventional docetaxel. Clinical activity was noted in multiple tumor types. The recommended phase II dose of BIND-014 is 60 mg/m(2) every three weeks or 40 mg/m(2) weekly. Clin Cancer Res; 22(13); 3157-63. ©2016 AACR.
Insights
This Phase I trial shows BIND-014, a novel nanoparticle delivering docetaxel, is safe and effective against various advanced solid tumors. It demonstrated a unique pharmacokinetic profile and clinical activity, warranting further investigation.
Area of Science:
- Oncology
- Nanomedicine
- Pharmacology
Background:
- Advanced solid tumors represent a significant unmet medical need.
- Docetaxel is a widely used chemotherapeutic agent with limitations in delivery and toxicity.
- Targeted drug delivery systems aim to improve efficacy and reduce side effects of chemotherapy.
Purpose of the Study:
- To evaluate the safety, pharmacokinetics, and antitumor activity of BIND-014, a novel prostate-specific membrane antigen (PSMA)-targeted nanoparticle containing docetaxel.
- To determine the recommended Phase II dose for BIND-014.
Main Methods:
- A first-in-human Phase I clinical trial.
- Patients with advanced solid tumors received BIND-014 intravenously every three weeks or weekly.
- Dose escalation was performed to determine safety and pharmacokinetic profiles.
Main Results:
- BIND-014 was well-tolerated with manageable toxicities, including neutropenia, fatigue, anemia, alopecia, and diarrhea.
- A dose-linear pharmacokinetic profile was observed, with prolonged circulation of docetaxel-encapsulated nanoparticles.
- Clinical activity was noted in multiple tumor types, including complete and partial responses in cervical, ampullary adenocarcinoma, non-small cell lung, prostate, breast, and gastroesophageal cancers.
Conclusions:
- BIND-014 exhibits a favorable safety profile and a unique pharmacokinetic profile compared to conventional docetaxel.
- Clinical activity was observed across various tumor types, irrespective of PSMA expression.
- The recommended Phase II doses are 60 mg/m(2) every three weeks or 40 mg/m(2) weekly.
