Data support a planned clinical trial of NX-2127 in B-cell malignancies
SAN FRANCISCO, CA, USA I December 07, 2020 INurix Therapeutics, Inc.(Nasdaq: NRIX), a biopharmaceutical company developing targeted protein modulation drugs, today announced the presentation of key preclinical data from its lead program, NX-2127, for the potential treatment of B-cell malignancies, at the 62nd American Society of Hematology (ASH) Annual Meeting and Exposition. Supported by these data, Nurix plans to initiate a Phase 1 clinical trial of orally administered NX-2127 in patients with relapsed or refractory non-Hodgkin’s lymphoma (NHL) and chronic lymphocytic leukemia (CLL) in the first half of 2021.
“The data presented at ASH demonstrate the unique dual properties of NX-2127 which is designed to overcome treatment failures including resistance to approved agents while simultaneously activating additional cancer-fighting immune cells,” said Robert Brown, M.D., vice president of clinical development of Nurix. “We look forward to advancing our novel targeted protein dual degrader to the clinic for patients with B-cell malignancies who have failed to respond to currently available therapies.”
NX-2127 catalyzes proteasomal degradation of Bruton’s tyrosine kinase (BTK), an enzyme involved in B-cell development, differentiation and signaling that is critical for proliferation and survival of lymphoma and leukemia cells in many B-cell malignancies, including NHL and CLL. Inhibitors of BTK, such as ibrutinib, are approved for treatment of B-cell cancers, however specific mutations can arise in the BTK protein that confer resistance to these agents, thereby reducing their efficacy. Degradation of BTK has the potential to overcome resistance in patients harboring such mutations in BTK. In addition, NX-2127 catalyzes degradation of a transcription factor involved in regulating T-cell function, resulting in T-cell activation in a similar fashion to immunomodulatory imide drugs (IMiD) that have demonstrated efficacy in some aggressive B-cell malignancies.
The data presented at ASH demonstrate that NX-2127 catalyzes potent and selective degradation of both wild type and ibrutinib-resistant mutant BTK (BTKC481S) in lymphoma cell lines and inhibits their growth. In addition, NX-2127 treatment of normal human T-cells results in their activation with similar potency to commercially available IMiDs, pomalidomide and lenalidomide, as measured by degradation of the transcription factor Aiolos and production of IL-2. Notably, orally administered NX-2127 results in potent anti-tumor effects in mouse xenograft models and rapid and near complete BTK degradation in preclinical testing in non-human primates with once-daily dosing.
About Nurix Therapeutics, Inc.
Nurix Therapeutics is a biopharmaceutical company focused on the discovery, development, and commercialization of small molecule therapies designed to modulate cellular protein levels as a novel treatment approach for cancer and immune disorders. Leveraging Nurix’s extensive expertise in E3 ligases together with its proprietary DNA-encoded libraries, Nurix has built DELigase, an integrated discovery platform to identify and advance novel drug candidates targeting E3 ligases, a broad class of enzymes that can modulate proteins within the cell. Nurix’s drug discovery approach is to either harness or inhibit the natural function of E3 ligases within the ubiquitin proteasome system to selectively decrease or increase cellular protein levels. Nurix’s wholly owned pipeline comprises targeted protein degraders of Bruton’s tyrosine kinase, a B-cell signaling protein, and inhibitors of Casitas B-lineage lymphoma proto-oncogene-B, an E3 ligase that regulates T cell activation. Nurix is headquartered in San Francisco, California. For more information, please visit http://www.nurix.com.
SOURCE: Nurix Therapeutics
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Data support a planned clinical trial of NX-2127 in B-cell malignancies
SAN FRANCISCO, CA, USA I December 07, 2020 INurix Therapeutics, Inc.(Nasdaq: NRIX), a biopharmaceutical company developing targeted protein modulation drugs, today announced the presentation of key preclinical data from its lead program, NX-2127, for the potential treatment of B-cell malignancies, at the 62nd American Society of Hematology (ASH) Annual Meeting and Exposition. Supported by these data, Nurix plans to initiate a Phase 1 clinical trial of orally administered NX-2127 in patients with relapsed or refractory non-Hodgkin’s lymphoma (NHL) and chronic lymphocytic leukemia (CLL) in the first half of 2021.
“The data presented at ASH demonstrate the unique dual properties of NX-2127 which is designed to overcome treatment failures including resistance to approved agents while simultaneously activating additional cancer-fighting immune cells,” said Robert Brown, M.D., vice president of clinical development of Nurix. “We look forward to advancing our novel targeted protein dual degrader to the clinic for patients with B-cell malignancies who have failed to respond to currently available therapies.”
NX-2127 catalyzes proteasomal degradation of Bruton’s tyrosine kinase (BTK), an enzyme involved in B-cell development, differentiation and signaling that is critical for proliferation and survival of lymphoma and leukemia cells in many B-cell malignancies, including NHL and CLL. Inhibitors of BTK, such as ibrutinib, are approved for treatment of B-cell cancers, however specific mutations can arise in the BTK protein that confer resistance to these agents, thereby reducing their efficacy. Degradation of BTK has the potential to overcome resistance in patients harboring such mutations in BTK. In addition, NX-2127 catalyzes degradation of a transcription factor involved in regulating T-cell function, resulting in T-cell activation in a similar fashion to immunomodulatory imide drugs (IMiD) that have demonstrated efficacy in some aggressive B-cell malignancies.
The data presented at ASH demonstrate that NX-2127 catalyzes potent and selective degradation of both wild type and ibrutinib-resistant mutant BTK (BTKC481S) in lymphoma cell lines and inhibits their growth. In addition, NX-2127 treatment of normal human T-cells results in their activation with similar potency to commercially available IMiDs, pomalidomide and lenalidomide, as measured by degradation of the transcription factor Aiolos and production of IL-2. Notably, orally administered NX-2127 results in potent anti-tumor effects in mouse xenograft models and rapid and near complete BTK degradation in preclinical testing in non-human primates with once-daily dosing.
About Nurix Therapeutics, Inc.
Nurix Therapeutics is a biopharmaceutical company focused on the discovery, development, and commercialization of small molecule therapies designed to modulate cellular protein levels as a novel treatment approach for cancer and immune disorders. Leveraging Nurix’s extensive expertise in E3 ligases together with its proprietary DNA-encoded libraries, Nurix has built DELigase, an integrated discovery platform to identify and advance novel drug candidates targeting E3 ligases, a broad class of enzymes that can modulate proteins within the cell. Nurix’s drug discovery approach is to either harness or inhibit the natural function of E3 ligases within the ubiquitin proteasome system to selectively decrease or increase cellular protein levels. Nurix’s wholly owned pipeline comprises targeted protein degraders of Bruton’s tyrosine kinase, a B-cell signaling protein, and inhibitors of Casitas B-lineage lymphoma proto-oncogene-B, an E3 ligase that regulates T cell activation. Nurix is headquartered in San Francisco, California. For more information, please visit http://www.nurix.com.
SOURCE: Nurix Therapeutics
Post Views: 132
