CG-806... starts the long trek..

[Cllcanada]

Aptose Biosciences announced that it has submitted an Investigational New Drug (IND) application for CG-806 to the U.S. Food and Drug Administration (FDA) requesting approval to initiate its Phase 1 clinical trial program. CG-806 is an oral, first-in-class small molecule inhibitor of all known forms of FLT3 and BTK kinases being developed for the treatment of patients with select hematologic malignancies, including chronic lymphocytic leukemia (CLL/SLL) and non-Hodgkin’s lymphomas, as well as for patients with relapsed/refractory acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).

Pending regulatory allowance, Aptose plans to conduct a Phase 1 trial with orally administered CG-806 in patients with relapsed or refractory B cell malignancies, including CLL/SLL and non-Hodgkin lymphomas (NHL) who failed or are intolerant to standard therapies. Pending the collection of predictive pharmacokinetic data in humans, Aptose would seek allowance from the FDA to move into the AML/MDS patient population in a separate Phase1 trial. The initial goal of both trials is to evaluate safety, tolerability and pharmacokinetics of CG-806 in these patient populations.

CG-806 is an oral, first-in-class pan-FLT3/pan-BTK multi-cluster kinase inhibitor. This small molecule, in-licensed from CrystalGenomics Inc. in Seoul S. Korea, demonstrates potent inhibition of wild type and all mutant forms of FLT3 (including internal tandem duplication, or ITD, and mutations of the receptor tyrosine kinase domain and gatekeeper region), cures animals of acute myeloid leukemia (AML) tumors in the absence of toxicity in murine xenograft models, and represents a potential best-in-class therapeutic for patients with AML. Likewise, CG-806 demonstrates potent, non-covalent inhibition of the wild type and Cys481Ser (C481S) mutant forms of the BTK enzyme, as well as other oncogenic kinase pathways operative in B cell malignancies, suggesting CG-806 may be developed for various B cell malignancy patients (including CLL, MCL, DLBCL and others) that are resistant/refractory/intolerant to covalent BTK inhibitors. Because CG-806 targets key kinases/pathways operative in malignancies derived from the bone marrow, it is in development for B cell cancers and AML.

apnews.com/32367d970ef77dd7...

Company website

aptose.com/cg806/

[cllady01 Former Volunteer]

Chris, is that as broad a disease target for a medicine as it sounds to be or are there others that work already in place with that disease target?

[Cllcanada Top Poster CURE Hero in reply to cllady01]

Think.. super Imbruvica (ibrutinib) perhaps.. its a multi-cluster kinase inhibitor... a double whammy...

It targets BTK like Imbruvica (ibrutinib) and also FLT3... blocks two pathways...

uniprot.org/uniprot/P36888

This may help...

globenewswire.com/news-rele...

[cllady01 Former Volunteer in reply to Cllcanada]

The "Forward Looking Statements" is quite a disclaimer and one well-crafted and stated. Gives light to the circuitous path to clinic/market.

[Justasheet1 in reply to cllady01]

I wonder how much the attorneys charged to draw that statement up?

Jeff

[Cllcanada Top Poster CURE Hero in reply to Justasheet1]

LOTS X 3

[Ernest2]

Hi Chris,

Does the FLT3 relate mainly to AML (great to make progress there) or does it also help with CLL.

Its also the first time I remember something developed from S. Korea. Hope that is a good sign.

Best wishes,

Ernest

[Cllcanada Top Poster CURE Hero in reply to Ernest2]

FLT3 , remains to be seen in CLL... these are pilot trials, trying to see where the drug is best used.

South Korea has a Rituxan biosimilar, Truxima, just approved in the EU and is waiting final approval in the U.S. FDA

koreaherald.com/view.php?ud...