Comprehensive Report on AD-101 (Addpharma): A Micronized Raloxifene Formulation

1. Executive Summary

This report provides a comprehensive analysis of AD-101, a pharmaceutical product developed by Addpharma, Inc. of South Korea. AD-101 is an Incrementally Modified Drug (IMD) consisting of a novel low-dose (45mg) micronized formulation of raloxifene hydrochloride, an established Selective Estrogen Receptor Modulator (SERM). The primary indication for AD-101 (Addpharma) is postmenopausal osteoporosis.

Key findings indicate that Addpharma, Inc., a subsidiary of Yuhan Corporation, successfully developed AD-101 to address the poor bioavailability of conventional raloxifene. Through micronization and optimized formulation, the 45mg dose of AD-101 demonstrated pharmacokinetic bioequivalence to the conventional 60mg raloxifene dose in Phase I clinical trials conducted in healthy volunteers.[1] This achievement allowed for a streamlined development pathway, culminating in marketing authorization for AD-101 in South Korea in September 2019.[3] The intellectual property underpinning this innovation is primarily captured in South Korean patent KR102351931B1, which details the specific particle size and formulation characteristics of the 45mg raloxifene product.[4]

The development of AD-101 (Addpharma) exemplifies a focused IMD strategy, leveraging an existing, well-characterized active pharmaceutical ingredient (API) to deliver tangible improvements in drug delivery and dosing. This approach offers a potentially enhanced therapeutic option for patients and a distinct market position. It is critical to differentiate this raloxifene-based AD-101 from other investigational agents that may share the "AD-101" designation but possess entirely different APIs, mechanisms of action, and target indications, such as the AD-101 being developed by AmyriAD Therapeutics for Alzheimer's disease and HIV infections.[2]