CYT387

What is CYT387?

 

CYT387 is a novel oral JAK1/JAK2 inhibitor initially targeting the treatment of a group of hematological disorders known as myeloproliferative neoplasms (MPNs), also known as myeloproliferative disorders. Additional potential treatment indications for CYT387 include other MPNs, cancer (solid and liquid tumors), graft-vs-host disease, and inflammatory conditions.

 

CYT387 was developed by Australian biotech company Cytopia Research Pty Ltd, and is now part of the YM BioSciences development program.

 

How does CYT387 work?

 

CYT387 is a potent, selective JAK1/JAK2 inhibitor designed to suppress the over-activity of the mutant JAK2.
The compound possesses an excellent selectivity and safety profile with minimal off-target activities, favorable pharmacokinetic properties, a clean toxicological profile and the prospect of limited drug/drug interactions. Preliminary data using samples derived from MPN patients have shown promising activity in suppressing the over-activity of the JAK2V617F mutant enzyme.




JAK2 in myeloproliferative neoplasms

MPNs are debilitating, and potentially fatal, diseases of blood cell production. MPNs such as polycythemia vera (PV), essential thrombocythemia (ET) and myelofibrosis (MF) are disorders for which there are limited and poorly efficacious therapeutic options. In an in vivo model of MPNs, CYT387 showed excellent activity, essentially reversing a number of the hallmarks of the disease.

More information about myeloproliferative neoplasms can be found at www.mpdfoundation.org.

JAK2 in cancer

JAK2 and its related biochemical pathways are now known to play a key role in the proliferation of certain types of cancer cells such as prostate, breast, head & neck, lung, ovarian, renal cell, glioma, pancreatic and liver cancers, and hematological cancers such as multiple myeloma, lymphoma and leukemia. Preclinical research is underway to examine the activity of CYT387 in these indications.

 

Clinical trials with CYT387

 

The compound is currently being studied in a Phase I/II clinical trial at Mayo Clinic in patients with myelofibrosis.

 

Availability of CYT387

 

CYT387 is available through participation in ongoing clinical trials.