Approaches for Estimating the Clinical Starting Dose of New Dosage Forms: An Example of a Long-Acting Injectable Formulation of Finasteride

December 2022 in “ International Journal of Pharmaceutics ”

Dong Wook Kang, Ju Hee Kim, Hea-Young Cho

finasteride long-acting injectable NOAEL-based pharmacokinetically-guided PK/PD model-based Propecia LAI

TLDR The best starting dose for a new finasteride injection is 16.80 mg.

The study aimed to predict the first-in-human (FIH) dose of a long-acting injectable (LAI) formulation of finasteride using three approaches: NOAEL-based, pharmacokinetically-guided, and PK/PD model-based. The NOAEL-based approach estimated the highest starting dose at 81.06 mg, while the PK/PD model-based approach suggested the most optimal starting dose at 16.80 mg. The study concluded that these methodologies could serve as a basis for Investigational New Drug (IND) applications for new dosage forms.

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Research cited in this study

6 / 6 results

Pharmacokinetic-Pharmacodynamic Modeling Approach for Dose Prediction of the Optimal Long-Acting Injectable Formulation of Finasteride

research Pharmacokinetic-Pharmacodynamic Modeling Approach for Dose Prediction of the Optimal Long-Acting Injectable Formulation of Finasteride

6 citations, March 2021 in “International Journal of Pharmaceutics”

Optimal long-acting finasteride injection dose found: 16.8 mg, effective for one month.

A Novel Finasteride 0.25% Topical Solution for Androgenetic Alopecia: Pharmacokinetics and Effects on Plasma Androgen Levels in Healthy Male Volunteers

research A Novel Finasteride 0.25% Topical Solution for Androgenetic Alopecia: Pharmacokinetics and Effects on Plasma Androgen Levels in Healthy Male Volunteers

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New finasteride solution effectively reduces baldness-causing hormone, potentially with fewer side effects.

research Saturable Binding of Finasteride to Steroid 5α-Reductase as Determinant of Nonlinear Pharmacokinetics

16 citations, January 2010 in “Drug Metabolism and Pharmacokinetics”

Finasteride's effect on hair loss and prostate enlargement depends on its binding to an enzyme, with maximum impact at 0.2 mg dose.

A Model for the Turnover of Dihydrotestosterone in the Presence of the Irreversible 5α-Reductase Inhibitors GI198745 and Finasteride

research A Model for the Turnover of Dihydrotestosterone in the Presence of the Irreversible 5α-Reductase Inhibitors GI198745 and Finasteride

60 citations, December 1998 in “Clinical Pharmacology & Therapeutics”

Both drugs lower DHT levels, with GI198745 being more effective.

research Clinical Pharmacokinetics and Pharmacodynamics of Finasteride

93 citations, January 1996 in “Clinical Pharmacokinectics”

Finasteride helps regrow hair and shrink prostate by reducing DHT, with some sexual side effects.

research Effects of Finasteride (MK-906), a 5α-Reductase Inhibitor, on Circulating Androgens in Male Volunteers

147 citations, April 1990 in “The Journal of Clinical Endocrinology and Metabolism”

Finasteride safely lowers DHT levels without affecting testosterone.

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

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

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research Pharmacokinetic-Pharmacodynamic Modeling Approach for Dose Prediction of the Optimal Long-Acting Injectable Formulation of Finasteride

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research A Microfluidic Application for Mass Production of Drug-Loaded Polymeric Microspheres for a Long-Acting Injectable With IVL-DrugFluidic, a Novel Microfluidic Microsphere Manufacturing Platform Technology

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research Development and Evaluation of Crystalline Inclusion Complex of Finasteride Using Electrospraying as a Novel Approach

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Approaches for Estimating the Clinical Starting Dose of New Dosage Forms: An Example of a Long-Acting Injectable Formulation of Finasteride

Research cited in this study

research Pharmacokinetic-Pharmacodynamic Modeling Approach for Dose Prediction of the Optimal Long-Acting Injectable Formulation of Finasteride

research A Novel Finasteride 0.25% Topical Solution for Androgenetic Alopecia: Pharmacokinetics and Effects on Plasma Androgen Levels in Healthy Male Volunteers

research Saturable Binding of Finasteride to Steroid 5α-Reductase as Determinant of Nonlinear Pharmacokinetics

research A Model for the Turnover of Dihydrotestosterone in the Presence of the Irreversible 5α-Reductase Inhibitors GI198745 and Finasteride

research Clinical Pharmacokinetics and Pharmacodynamics of Finasteride

research Effects of Finasteride (MK-906), a 5α-Reductase Inhibitor, on Circulating Androgens in Male Volunteers

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