rezatapopt (** Generic name only (investigational); no commercial brand names yet established. **)

Other Medications

EU Experimental ES Not available 2 Clinical Trials

Description

Rezatapopt is an experimental (investigational) oral medication currently being studied in clinical trials for certain advanced cancers. It is being investigated as a potential treatment for colorectal cancer patients whose tumors have a specific mutation in the TP53 gene, known as the Y220C mutation. This mutation is found in a small percentage of colorectal cancers. Rezatapopt belongs to a class of drugs called p53 reactivators. It is being studied both on its own (monotherapy) and in combination with other cancer drugs like pembrolizumab (an immunotherapy drug). The goal of these trials is to determine the right dose, how safe it is, and if it can shrink tumors or slow their growth in patients with this specific TP53 mutation. It is not yet approved for use in colorectal cancer or any other cancer.

Mechanism of Action

Rezatapopt is designed to target and 'reactivate' the p53 protein within cancer cells. The p53 protein is often called the 'guardian of the genome' because it helps control cell growth and can trigger cell death (apoptosis) if DNA damage is detected. However, certain mutations, like the TP53 Y220C mutation, can prevent the p53 protein from working correctly. Rezatapopt is specifically designed to bind to and restore the function of the p53 protein when this particular Y220C mutation is present, potentially helping the cancer cell self-destruct or become more sensitive to other treatments.

Side Effects

Rezatapopt is still in early-phase clinical trials (Phase 1). Therefore The full range of potential side effects is still being evaluated. Information from the trials (like NCT04585750) indicates that common side effects observed in early studies include fatigue Nausea Diarrhea Decreased appetite And constipation. More serious side effects have also been reported. As the drug is still investigational Side effects are still being carefully monitored and characterized in ongoing trials.

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT07372625 Phase 1
Recruiting
A Study to Investigate the Effects of Multiple Doses of Rezatapopt on the Pharmacokinetics of Metformin, Rosuvastatin, Repaglinide, and Midazolam in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation.
United States
NCT04585750 Phase 1
Recruiting
The Evaluation of PC14586 in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation (PYNNACLE)
United States, Australia, France, Germany, Italy, Singapore, South Korea, Spain,