NCT01765478

Safety,PK/PD, Food Effect Study of Orally Administered HM71224 in Healthy Adult Male Volunteers

A Phase1 Study, to Determine the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Food Effect of Single and Multiple Doses of Orally Administered HM71224 in Healthy, Adult Male Volunteers

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 62 (estimated)
• Sponsor: Hanmi Pharmaceutical Company Limited · Industry
• Sex: Male
• Age: 18 Years – 65 Years
• Healthy volunteers: Accepted

Summary

HM71224 is a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK). BTK is a member of the Tec family of non-receptor protein tyrosine kinases. BTK is mostly expressed in hematopoietic cells such as B cells, mast cells and macrophages. BTK plays key roles in multiple cell signaling pathways including B-Cell Receptor (BCR) and Fc receptor (FcR) signaling cascades and is an essential mediator not only in B-cell dependent but also in myeloid cell dependent inflammatory arthritis. HM71224 has been selected as a novel therapeutic agent for the treatment of autoimmune diseases such as rheumatoid arthritis (RA). In view of the above, further development of HM71224 for the treatment of RA is warranted. In this first-in-man (FIM) study, a single and multiple dose escalation design will be employed, in which the primary objective is to evaluate the safety and tolerability of the compound. The biomarkers included as pharmacodynamic (PD) variables are chosen as they are indicators for any effects of HM71224 on the expected mode of action (pBTK, pPLCγ, and pERK).

Detailed description

Primary objective * To evaluate the safety and tolerability, and if possible maximum tolerated dose (MTD) of HM71224 after single and multiple ascending dose administration in healthy subjects. Secondary objective * To determine the PK of HM71224 and selected metabolites (M1 and M2) following single and multiple oral dose administration of HM71224. * To assess the PD effects of HM71224 on the biomarkers pBTK, pPLCγ, and pERK. * To assess whether the PK of HM71224 is affected by food.

Conditions

• Rheumatoid Arthritis

Interventions

Type	Name	Description
DRUG	HM71224 single ascending dose
DRUG	HM71224 food effect
DRUG	HM71224 Multiple ascending dose

Timeline

• Start date: 2013-01-01
• Primary completion: 2014-11-01
• Completion: 2014-11-01
• First posted: 2013-01-10
• Last updated: 2015-05-18

Locations

1 site across 1 country: Netherlands