Aptose Biosciences is a clinical-stage biotechnology company focused on developing precision oncology therapies, particularly for hematologic malignancies. The company’s pipeline includes small molecule cancer therapeutics designed to achieve single-agent efficacy while enhancing the effectiveness of existing anti-cancer treatments without causing overlapping toxicities. Their lead drug candidate, Tuspetinib, is a potent oral myeloid kinase inhibitor targeting key kinases involved in myeloid malignancies, such as acute myeloid leukemia (AML). Additionally, Luxeptinib, another candidate, serves as a lymphoid kinome inhibitor, effectively targeting both wildtype and mutant forms of BTK, which are critical in various B-cell malignancies, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).

The company is currently conducting multiple clinical trials to evaluate the safety and efficacy of its investigational drug candidates. Tuspetinib is undergoing a Phase 1/2 trial for relapsed or refractory AML, while Luxeptinib is in Phase 1a/b trials for B-cell malignancies and AML/MDS. Aptose's approach emphasizes the development of targeted therapies that can be used alone or in combination with other treatments, aiming to address unmet clinical needs in oncology and improve patient outcomes through precision medicine.

Canada

Aptose Biosciences is a science-driven clinical-stage biotechnology company developing first-in-class targeted agents to address unmet clinical need in multiple hematologic malignancies.

CG-806, our oral mutation-agnostic FLT3/BTK inhibitor, is being developed for the treatment of patients with certain B-cell malignancies, including chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), and certain non-Hodgkin’s lymphomas (NHL) who are resistant or intolerant to conventional treatments. 

CG-806 is also being developed for the treatment of patients with relapsed or refractory acute myeloid leukemia (AML), including the emerging populations resistant to approved targeted therapies.

APTO-253, our first-in-class MYC Inhibitor, is being developed for the treatment of patients with relapsed or refractory acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).

Cancer

Hematologic Diseases

Lymphatic Diseases

Aptose Biosciences

Acute myeloid leukemia

Leukemia

Relapsed/refractory acute myeloid leukemia

HM43239 is an oral, once-daily, highly potent myeloid kinome inhibitor (MKI) designed to target key kinases operative in myeloid malignancies.
(myeloid kinase inhibitor)&nbsp;

Tuspetinib mono/combo w/ Venetoclax

Chronic lymphocytic leukemia

Non-Hodgkin lymphoma

CG-806 is an oral, first-in-class pan-FLT3/pan-BTK &nbsp;multi-cluster kinase inhibitor and is in a Phase 1 clinical trial for &nbsp;the treatment of hematologic malignancies. This small molecule, &nbsp;in-licensed from CrystalGenomics Inc. in Seoul, South Korea, &nbsp;demonstrates potent inhibition of wild type and all mutant forms of FLT3 &nbsp;(including internal tandem duplication, or ITD, and mutations of the &nbsp;receptor tyrosine kinase domain and gatekeeper region), cures animals of &nbsp;AML in the absence of toxicity in murine xenograft models, and &nbsp;represents a potential best-in-class therapeutic for patients with AML &nbsp;and other hematologic malignancies. Likewise, CG-806 demonstrates &nbsp;potent, non-covalent inhibition of the wild type and Cys481Ser (C481S) &nbsp;mutant forms of the BTK enzyme, as well as other oncogenic kinase &nbsp;pathways operative in B cell malignancies, suggesting CG-806 may be &nbsp;developed for various B cell malignancy patients (including CLL/SLL, FL, &nbsp;MCL, DLBCL and others) that are resistant/refractory/intolerant to &nbsp;covalent or other non-covalent BTK inhibitors. Because CG-806 targets &nbsp;key kinases/pathways operative in malignancies derived from the bone &nbsp;marrow, it is in development for B-cell cancers and AML.
<a href="https://www.aptose.com/news-media/press-releases/detail/149/aptose-doses-first-cll-patient-in-phase-1-study-of-cg-806">Source</a>

Luxeptinib (CG-806)

Tuspetinib / Venetoclax / Azacitidine  triplet

Myelodysplastic syndrome

APTO-253 as a Small Molecular MYC Inhibitor: APTO-253 does not target directly the MYC protein, but rather binds directly and selectively to a regulatory motif in the promoter of the MYC oncogene and dramatically down-regulates expression of the MYC protein in tumor cells, leading to apoptotic cell death. Thus, APTO-253 may serve as a safe and effective MYC inhibitor for MYC-driven or MYC-dependent tumors that combines well with other anti-tumor agents.

APTO-253 

B-cell malignancies

HM43239 is an oral, once-daily, highly potent myeloid kinome inhibitor (MKI) designed to target key kinases operative in myeloid malignancies.

Aptose Biosciences

Company Details