Discover AZD5991: A Breakthrough Mcl-1 Inhibitor for Hematologic Cancers
Explore the potent preclinical efficacy of AZD5991, a novel Mcl-1 inhibitor targeting apoptosis in blood cancers.
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Mcl-1 Inhibitor AZD5991
AZD5991 is a rationally designed macrocyclic molecule exhibiting high selectivity and affinity for Mcl-1, a key protein in cell survival pathways. Its mechanism involves direct binding to Mcl-1, triggering rapid apoptosis in cancer cells, particularly those with high Mcl-1 expression like myeloma and acute myeloid leukemia. This is achieved by activating the Bak-dependent mitochondrial apoptotic pathway.
- Investigate the discovery of Mcl-1-specific inhibitor AZD5991 and its potent preclinical activity in targeting leukemia.
- Understand the mechanism of AZD5991, which induces rapid apoptosis by activating the Bak-dependent mitochondrial apoptotic pathway.
- Learn about the drug discovery and development process for AZD5991, highlighting its journey to clinical trials.
- Explore the potential of Mcl-1 inhibitor drug discovery in treating hematological malignancies and other cancers.
Key Advantages
High Selectivity and Affinity
AZD5991 demonstrates exceptional selectivity for Mcl-1 over other Bcl-2 family proteins, a crucial aspect of its targeted approach in cancer therapy.
Potent Anti-tumor Efficacy
Preclinical studies show AZD5991 exhibiting potent anti-tumor activity, leading to complete tumor regression in multiple myeloma and acute myeloid leukemia models.
Combination Therapy Potential
The drug shows promise when used in combination with agents like bortezomib and venetoclax, enhancing anti-tumor responses and potentially overcoming resistance mechanisms.
Key Applications
Multiple Myeloma Treatment
AZD5991 is being investigated for its efficacy in treating multiple myeloma, a cancer that relies on Mcl-1 for survival.
Acute Myeloid Leukemia Therapy
The compound shows significant promise in preclinical models of acute myeloid leukemia, suggesting its potential as a therapeutic agent.
Hematologic Malignancies
AZD5991's mechanism of action makes it a candidate for treating a broader range of hematologic malignancies where Mcl-1 plays a critical role.
Pharmaceutical Research & Development
AZD5991 serves as a valuable tool in understanding Mcl-1 biology and advancing the field of protein-protein interaction inhibitor design.