Carna has leveraged its expertise in small molecule drug discovery to establish an innovative product pipeline focused on cancer and immune disorders. We achieve success by coupling our deep understanding of cell signaling with our extensive drug discovery expertise to generate therapeutics that provide new treatment options for patients with high unmet medical needs.
Pipeline in Development
- monzosertib (CDC7 inhibitor)
- Solid Tumors/Hematological Malignancies
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IND-enabling Early Clinical Late Clinical
- monzosertib (AS-0141)
- Monzosertib is a potent, selective, orally bioavailable small molecule inhibitor of cell division cycle 7 (CDC7) kinase, originally discovered by Carna. Monzosertib exhibited a potent anti-proliferative activity against various cancer cell lines including solid and blood cancers with minimal effects against normal cells. In several human tumor xenograft models, oral administration of monzosertib demonstrated strong anti-tumor efficacy. Monzosertib is currently being evaluated in an open-label Phase 1 study in patients with advanced, metastatic, relapsed or refractory malignancies.
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- docirbrutinib (wild-type & pan-mutant BTK inhibitor)
- Hematological Malignancies
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IND-enabling Early Clinical Late Clinical
- docirbrutinib (AS-1763)
- Docirbrutinib is a highly selective, orally bioavailable, non-covalent pan-inhibitor of wild type and mutant Bruton's tyrosine kinases (BTK) for the treatment of chronic lymphocytic leukemia(CLL) and other B-cell malignancies. Covalent BTK inhibitors including ibrutinib are key therapeutic options for patients with B-cell malignancies. However, patients are reported to develop resistance during the treatment due to substitution of cysteine residue at 481 position with serine (C481S mutation) in BTK, which reduces the efficacy of the covalent BTK inhibitors. In addition, the emergence of other types of resistance mutations to non-covalent BTK inhibitor, recently approved pirtobrutinib, has been reported. Docirbrutinib potently inhibited both wild type and those mutant BTKs, strongly suggesting that docirbrutinib will be a new therapeutic option for treating patients with B-cell malignancies who have developed resistance to currently approved BTK inhibitors.
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- sofnobrutinib (BTK inhibitor)
- Inflammatory/Immune disorders
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IND-enabling Early Clinical Late Clinical
- sofnobrutinib (AS-0871)
- Sofnobrutinib is a non-covalent Bruton's tyrosine kinases (BTK) inhibitor designed to bind preferentially to non-activated form of BTK with high selectivity, currently in clinical development for inflammatory and immune disorders. In in vitro experiments, sofnobrutinib strongly inhibited B cell and basophil activation and suppressed production of inflammatory cytokines such as TNF-α, IL-17, MCP-1 and IL-6 in human blood. Oral administration of sofnobrutinib demonstrated the excellent therapeutic effects in a mouse model of collagen-induced arthritis. In addition, sofnobrutinib prevented IgE-mediated skin inflammation in mice and rats.
The Phase 1 single ascending dose (SAD) study and multiple ascending dose (MAD) study of sofnobrutinib in healthy volunteers have been completed. Currently seeking strategic partners to accelerate late-stage development. - LEARN MORE
We are actively pursuing early discovery programs to create next wave of clinical pipeline.
Partnered programs and collaborations
- DGKα inhibitor
- Partner:
- Territory: Worldwide
- In June 2019, Carna licensed Gilead Sciences worldwide rights to develop and commercialize small molecule compounds in immuno-oncology. In December 2023, Gilead initiated the Phase 1 study of GS-9911, an investigational DGKα inhibitor, developed by Gilead under the license and research collaboration. The details of the Phase 1 study of GS-9911 targeting patients with solid tumors can be found at Gilead’s website.
- Undisclosed Target
- Partner:
- Territory: Worldwide
- Carna and Sumitomo Pharma are conducting a joint research to discover novel kinase inhibitors to treat psychiatric and neurological disorders.