Acoziborole (Figure 1), an oxaborole-6 carboxamide, is being developed as an oral single dose treatment for Human African trypanosomiasis (also called "sleeping sickness"). As part of the overall development programme, the mass balance, pharmacokinetics, metabolism and excretion of acoziborole were studied in an open-label, phase 1 study. This poster will describe the mass balance and clinical safety assessments from the human ADME study. 

Acoziborole, an oxaborole-6 carboxamide, is being developed as an oral single dose treatment for Human African Trypanosomiasis. This poster will describe the metabolite characterization investigations following the human ADME studying a microdose of [14C]-Acoziborole. 

Acoziborole, an oxaborole-6 carboxamide, is being developed as an oral single dose treatment for Human African trypanosomiasis (also called "sleeping sickness"). As part of the overall development programme, the mass balance, pharmacokinetics, metabolism and excretion of acoziborole were studied in an open-label, clinical phase 1 study in six healthy male subjects. This poster describes the radiolabelling and purification of [14C]acoziborole as a GMP radiolabelled drug substance to support the human metabolism investigation. 

This is part of a series of 3 posters presented at ISSX 2024: 

Investigation of the Matabolite Profile of Acoziborole in Plasma Urine and Fecal Homogenate Samples Using UPLC-MS Fractionation Followed by AMS Analysis | Quotient Sciences

A Single Dose Study to Assess the Mass Balance Recovery, Absorption, Metabolism, and Excretion of [14C]-Acoziborole in Healthy Male Subjects After Oral Dosing | Quotient Sciences

Tackling the preclinical exposure challenge: Explore Quotient Sciences' preclinical services in drug development.

Drug solubility and bioavailability challenges are omnipresent in the pharmaceutical industry today, with over 80% of new drugs classified as poorly soluble relative to human dose requirements. Even before entering clinical evaluation stages, new therapeutics must overcome higher solubility hurdles required for concomitant non-GLP PK and initial dose range finding (DRF) studies where a linear dose-exposure relationship is required to justify further development effort and financial expenditure.