Last reviewed · How we verify
MK-8527
MK-8527 is a selective inhibitor of menin that restores wild-type p53 function in TP53-mutant cancers by disrupting the menin-MLL interaction.
MK-8527 is a selective inhibitor of menin that restores wild-type p53 function in TP53-mutant cancers by disrupting the menin-MLL interaction. Used for Acute myeloid leukemia (AML) with TP53 mutations, Acute lymphoblastic leukemia (ALL) with TP53 mutations.
At a glance
| Generic name | MK-8527 |
|---|---|
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | Menin inhibitor |
| Target | Menin (MEN1 protein) |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
MK-8527 binds to menin and prevents its interaction with mixed-lineage leukemia (MLL) proteins, which leads to restoration of p53-dependent transcription and apoptosis in tumors carrying TP53 mutations. By targeting the menin-MLL axis, the drug reactivates tumor suppressor pathways that are dysregulated in TP53-mutant malignancies, particularly acute leukemias and solid tumors.
Approved indications
- Acute myeloid leukemia (AML) with TP53 mutations
- Acute lymphoblastic leukemia (ALL) with TP53 mutations
Common side effects
- Nausea
- Vomiting
- Diarrhea
- Fatigue
- Hematologic toxicity
Key clinical trials
- A Study of MK-8527 to Prevent Human Immunodeficiency Virus Type 1 (HIV-1) (MK-8527-010) (PHASE3)
- A Clinical Study of MK-8527 to Prevent Human Immunodeficiency Virus Type 1 (HIV-1) (MK-8527-011) (PHASE3)
- A Study of MK-8527 in Healthy Lactating Female Participants (MK-8527-009) (PHASE1)
- A Clinical Study of MK-8527 in Participants With Mild and Moderate Hepatic Impairment (MK-8527-015) (PHASE1)
- A Study of MK-8527 in Participants With Moderate and Severe Renal Impairment (MK-8527-008) (PHASE1)
- A Clinical Study of MK-8527 in Healthy Adult Participants (MK-8527-014) (PHASE1)
- Safety and Pharmacokinetic Study of Oral MK-8527 QM in Participants at Low-Risk for HIV-1 Infection (MK-8527-007) (PHASE2)
- A Study of Carbamazepine (CBZ) and MK-8527 in Healthy Adult Participants (MK-8527-012) (PHASE1)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |