Potrasertib

A selective inhibitor of protein kinase AKT

Potrasertib
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Potrasertib is a small molecule inhibitor that selectively targets the protein kinase AKT, which is a key component of the PI3K/AKT/mTOR pathway. This pathway is crucial for regulating cell growth, survival, and metabolism, and is often dysregulated in various types of cancer.

Mechanism of Action

Potrasertib functions by inhibiting the activity of AKT, a serine/threonine-specific protein kinase. AKT plays a pivotal role in multiple cellular processes, including glucose metabolism, apoptosis, cell proliferation, and transcription. By inhibiting AKT, potrasertib disrupts these processes, which can lead to reduced tumor cell proliferation and increased apoptosis in cancer cells.

Clinical Development

Potrasertib has been investigated in several clinical trials for its potential use in treating different types of cancer. The drug's ability to inhibit AKT makes it a promising candidate for targeting tumors that exhibit hyperactivation of the PI3K/AKT/mTOR pathway. Clinical trials have focused on evaluating the safety, tolerability, and efficacy of potrasertib in patients with advanced solid tumors.

Pharmacokinetics

The pharmacokinetic profile of potrasertib involves its absorption, distribution, metabolism, and excretion. As a small molecule inhibitor, potrasertib is designed to be orally bioavailable, allowing it to be administered in pill form. The drug is metabolized primarily in the liver and excreted through the kidneys.

Potential Side Effects

As with many targeted cancer therapies, potrasertib may cause a range of side effects. Common side effects observed in clinical trials include fatigue, nausea, diarrhea, and rash. More serious adverse effects may include hyperglycemia, due to the role of AKT in glucose metabolism, and liver function abnormalities.

Research and Future Directions

Ongoing research is focused on identifying biomarkers that predict response to potrasertib, optimizing dosing regimens, and exploring combination therapies with other anticancer agents. The potential for potrasertib to be used in combination with other inhibitors of the PI3K/AKT/mTOR pathway is of particular interest, as this may enhance therapeutic efficacy and overcome resistance mechanisms.

Related Pages

• Protein kinase B
• PI3K/AKT/mTOR pathway
• Cancer therapy
• Targeted therapy