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A Phase I, Open-Label, Sequential, Single-Dose Clinical Trial to Evaluate the Pharmacokinetic, Pharmacodynamic, and Safety of IVL3001, a Finasteride-Based Novel Long-Acting Injection for Androgenetic Alopecia

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Abstract

Introduction

Hair loss is driven by multiple factors, including genetics. Androgenetic alopecia (AGA) is a condition in which treatments necessitate prolonged compliance with prescribed medications. We have developed IVL3001, a long-acting injectable (LAI) formulation of finasteride encapsulated within poly lactic-co-glycolic acid microspheres, to enhance the efficacy of the finasteride and to achieve consistent positive outcomes in adults. An open-label, sequential, single-dose phase I clinical trial was designed to evaluate the safety, pharmacokinetic (PK), and pharmacodynamic (PD) of IVL3001.

Methods

A total of 40 non-smoking, healthy adult males were divided into three cohorts where the IVL3001 group received a single subcutaneous injection of 12–36 mg IVL3001 and 1 mg finasteride (Propecia®) once daily for 28 days. The plasma concentrations of finasteride, dihydrotestosterone (DHT), and testosterone were measured using liquid chromatography–tandem mass spectrometry. The tolerability of the injections was assessed, and compartment models were developed to predict the effective dose and assess PK/PD profiles.

Results

IVL3001 and finasteride 1 mg tablets were well tolerated. IVL3001 showed consistent plasma concentrations without bursts or fluctuations. Consistent with its mechanism of action, IVL3001 reduced DHT levels. Simulation data showed that the administration of 12–36 mg of IVL3001 every 4 weeks achieved plasma concentrations similar to finasteride, with comparable DHT reduction.

Conclusion

The present study represents the first clinical trial to evaluate the safety, pharmacokinetic (PK), pharmacodynamic (PD), and tolerability of finasteride long-acting injectables (LAI) in adults. The rapid onset of action sustained effective drug concentration and the prolonged half-life of IVL3001 suggest that it offers multiple benefits over conventional oral formulations in terms of therapeutic response and compliance.

Trial Registration

ClinicalTrials.gov identifier, NCT04945226.

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Data Availability

The datasets acquired and examined in the present investigation are not publicly available due to confidentiality considerations.

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Acknowledgements

The authors thank the principal investigators and trial-site staff of Nucleus Network Pty Ltd, Brisbane, Australia. We thank the participants who generously agreed to participate in this clinical trial. We thank the Inventage Lab editorial department for their help with editing and formatting.

Funding

This study was supported by Inventage Lab, Seoul, Republic of Korea. The study rapid services fee, and open access fees were funded by Inventage Lab, Seoul, Republic of Korea. The study sponsor was involved in several aspects of the research, including experimental design, analysis, and interpretation of data, and drafting of manuscript.

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Authors and Affiliations

  1. Inventage Lab, 9F Uspace2B, 670, Daewangpangyo-ro, Bundang-gu, Seongnam-si, Gyeonggi-do, 13494, Republic of Korea

    Heesun Kim, Choongho Ryu, Mase Lee & Juhee Kim

  2. Department of Clinical Research Design & Evaluation, SAIHST, Sungkyunkwan University, Seoul, 06355, Republic of Korea

    Heesun Kim

  3. Laboratory Animal Resource Center, Korea Research Institute of Bioscience and Biotechnology, Cheongju, 28116, Republic of Korea

    Kyeong-Ryoon Lee

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  1. Heesun Kim
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Contributions

Inventage Lab research team conceived and designed the study. Heesun Kim and Juhee Kim participated in the trial inspection. Kyeong-Ryoon Lee and Choongho Ryu were involved in statistical analysis. Heesun Kim and Kyeong-Ryoon Lee. prepared the manuscript. All the authors read and approved the final manuscript.

Corresponding author

Correspondence to Juhee Kim.

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Conflict of Interest

The authors declare that the clinical trial is related to drugs with commercial significance, and no conflicts of interest may influence the objectivity and integrity of the study process.

Ethical Approval

This study was conducted according to the Therapeutic Goods Administration (TGA) and Human Research Ethics Committee (HREC) guidelines. The whole study was conducted in accordance with the provisions of the Helsinki Declaration and the standards for clinical trial management (GCP), and the protocol was registered at www.clinicaltrials.gov (NCT04945226; Reg date 2021–06-30). Potential volunteers completed signed informed consent and underwent a screening test prior to the trial.

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Kim, H., Ryu, C., Lee, M. et al. A Phase I, Open-Label, Sequential, Single-Dose Clinical Trial to Evaluate the Pharmacokinetic, Pharmacodynamic, and Safety of IVL3001, a Finasteride-Based Novel Long-Acting Injection for Androgenetic Alopecia. Adv Ther 41, 2936–2952 (2024). https://doi.org/10.1007/s12325-024-02890-1

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