Safety,PK/PD, Food Effect Study of Orally Administered HM71224 in Healthy Adult Male Volunteers
Status:
Completed
Trial end date:
2014-11-01
Target enrollment:
Participant gender:
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, pPLCĪ³, and pERK).