EARLY CLINICAL DEVELOPMENT PROGRAM, INCLUDING RESULTS OF A FIRST-IN-HUMAN TRIAL OF LIB-01, A NOVEL, FIRST IN CLASS POTENTIAL ORAL ERECTILE DYSFUNCTION DRUG WITH UNIQUE PHARMACODYNAMIC PROPERTIES

LIB-01 is a novel small molecule which is an analogue of the active component of a root bark long used in ethnopharmacology. The early clinical development program is presented, including results of the first-in-human safety and erectile function trial.

In the phase 1 trial, healthy men or men with ED (IIEF-EF score 11-25) underwent single or multiple ascending dosing (MAD) of LIB-01, respectively. Standard safety monitoring was performed for up to 28 days. In the MAD, erectile function was assessed by IIEF-EF and real-time RigiScan® with visual sexual stimulation. An open-ended question was asked on Day 14 and Day 28, to determine the pro-erectile effect duration.

In the Phase 2a trial, men with ED (IIEF-EF 11-25) receive LIB-01 or placebo and are evaluated for efficacy and safety for 8 weeks following a 3-day oral dosing. Efficacy assessments include IIEF-EF (week 4 and 8), Sexual Encounter Profile questions 2 and 3 (diary), and a Global Assessment Question (week 4 and 8).

In the phase 1 trial, the treatment-related AEs were few and mild and mostly GI related. There were no clinically significant findings on laboratory parameters, vital signs, or ECG.

Erectile rigidity increased in the LIB-01 treated group as measured by RigiScan® and erectile function was improved according to IIEF-EF. The effect was most pronounced in the 25 mg, 3-day dosing group with a mean increase in IIEF-EF of 7.8 and RigiScan® RAU of 3.8 (+40%) and 3.4 (+122%) for tip and base, respectively. All subjects reported a clinically meaningful improvement according to the IIEF-EF on Day 28.

LIB-01, a novel and first-in-class molecule, was safe and well tolerated when orally administered at single and multiple ascending doses. In addition, erectile function improvement was demonstrated with both IIEF-EF and RigiScan®. Most interestingly, a unique pharmacodynamic profile was observed with a duration of action of at least 28 days following a 3-day dosing. In conclusion, this compound has the potential to dramatically change the paradigm of ED management. The Phase 2a trial is ongoing.

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