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Researchers in the lab
Photo by Rhoda Baer

A dual kinase inhibitor is active against a range of hematologic malignancies, according to preclinical research.

Investigators found that ASN002, a SYK/JAK inhibitor, exhibited “potent” antiproliferative activity in leukemia, lymphoma, and myeloma cell lines.

ASN002 also inhibited tumor growth in mouse models of these malignancies and proved active against ibrutinib-resistant diffuse large B-cell lymphoma (DLBCL).

The investigators presented these results at the AACR Annual Meeting 2017 (abstract 4204).

The work was conducted by employees of Asana BioSciences, the company developing ASN002.

The investigators tested ASN002 in 178 cell lines and found the drug exhibited “strong antiproliferative activity” in a range of hematologic cancer cell lines, including:

  • Leukemia—HEL31, HL60, Jurkat, MOLM-13, and MOLM-16
  • Lymphoma—KARPAS-299, OCI-LY10, OCI-LY-19, Pfeiffer, Raji, Ramos, SU-DHL-1, SU-DHL-6, and SU-DHL-10
  • Myeloma—H929, JJN3, OPM2, and U266.

In addition, ASN002 was active against ibrutinib-resistant clones derived from the DLBCL cell line SU-DHL-6.

In a SU-DHL-6 xenograft model, the combination of ASN002 and ibrutinib was more effective than either compound alone.

The investigators also found that ASN002 alone demonstrated “strong tumor growth inhibition” in mouse models of DLBCL (Pfeiffer and SU-DHL-6), myeloma (H929), and erythroleukemia (HEL).

The team pointed out that ASN002 is currently under investigation in a phase 1/2 study of patients with B-cell lymphomas (DLBCL, mantle cell lymphoma, and follicular lymphoma) as well as solid tumors.

The investigators said that, to date, ASN002 has been well tolerated and has shown encouraging early evidence of clinical activity and symptomatic benefit in the lymphoma patients.


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