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Leukemia, myelomonocytic, chronic

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NEDD8-activating enzyme E1 catalytic subunit

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PEVONEDISTAT

S3AZD8D215

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

NEDD8-activating enzyme E1 catalytic subunit

Conditions:

Acute lymphoblastic leukemia

Myelodysplastic syndromes

Acute myeloid leukemia

Leukemia, myelomonocytic, chronic

Pevonedistat (MLN4924), discovered by Millennium, is a small molecule inhibitor of the NEDD8-Activating Enzyme (NAE), a key component of the protein homeostasis pathway. MLN4924 is a mechanism-based inhibitor of NAE and creates a covalent NEDD8-MLN49...

24 adduct catalyzed by the enzyme. The NEDD8-MLN4924 adduct resembles NEDD8 adenylate, the first intermediate in the NAE reaction cycle, but cannot be further utilized in subsequent intraenzyme reactions. The stability of the NEDD8-MLN4924 adduct within the NAE active site blocks enzyme activity, thereby accounting for the potent inhibition of the NEDD8 pathway by MLN4924. This drug is in phase II clinical trial for the treatment acute myeloid leukemia, chronic myelomonocytic leukemia and myelodysplastic syndromes. In addition in phase I for treatment acute lymphoblastic leukemia. The ability of MLN4924 to cross the blood-brain barrier, its low toxicity, and clinical efficacy in other cancers suggests that this drug is an attractive treatment against glioblastomas.

PEVONEDISTAT HYDROCHLORIDE

28I8PCX76B

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

NEDD8-activating enzyme E1 catalytic subunit

Conditions:

Acute lymphoblastic leukemia

Myelodysplastic syndromes

Acute myeloid leukemia

Leukemia, myelomonocytic, chronic

Pevonedistat (MLN4924), discovered by Millennium, is a small molecule inhibitor of the NEDD8-Activating Enzyme (NAE), a key component of the protein homeostasis pathway. MLN4924 is a mechanism-based inhibitor of NAE and creates a covalent NEDD8-MLN49...

24 adduct catalyzed by the enzyme. The NEDD8-MLN4924 adduct resembles NEDD8 adenylate, the first intermediate in the NAE reaction cycle, but cannot be further utilized in subsequent intraenzyme reactions. The stability of the NEDD8-MLN4924 adduct within the NAE active site blocks enzyme activity, thereby accounting for the potent inhibition of the NEDD8 pathway by MLN4924. This drug is in phase II clinical trial for the treatment acute myeloid leukemia, chronic myelomonocytic leukemia and myelodysplastic syndromes. In addition in phase I for treatment acute lymphoblastic leukemia. The ability of MLN4924 to cross the blood-brain barrier, its low toxicity, and clinical efficacy in other cancers suggests that this drug is an attractive treatment against glioblastomas.

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