Analysis of the targeted mechanism of action, indications and clinical efficacy of caposetinib tablets

In recent years, the AKT pathway has become an important focus in tumor research, and capivasertib (capivasertib) is a new generation of oral AKT inhibitors developed based on this mechanism. Its core targeting points are AKT1, AKT2, AKT3, which can effectively block the PI3K/AKT signaling pathway and inhibit tumor cell proliferation, metabolism and anti-apoptosis ability. Because breast cancer, ovarian cancer and other solid tumors are often accompanied by gene mutationsPIK3CA, AKT1, PTEN and other key molecules are dysregulated. By precisely inhibiting AKT activity, the drug significantly reduces the survival signal of tumor cells, thereby providing targeted therapeutic value for patients with specific molecular subtypes. Its mechanism features also include blocking the downstream mTOR pathway, interfering with sugar metabolism and DNA repair-related signals, so it also shows potential advantages in the context of drug resistance.

In terms of indications, capivasertib is currently mainly used in patients with hormone receptor-positive, HER2-negative advanced breast cancer, especially those with PIK3CA, AKT1 or PTEN People with altered gene mutations. Its treatment regimen combined with fulvestrant (Fulvestrant) has been proven to still have significant benefits in patients who are resistant to endocrine therapy. In addition, based on the broad-spectrum mechanism of action of the AKT pathway, the drug is also being clinically explored in a variety of tumors such as ovarian cancer, endometrial cancer, and prostate cancer, especially in tumor subtypes with PTEN deletion, showing more obvious sensitivity. With the further development of the precision treatment era, capivasertib is gradually expanding its application boundaries and is expected to become a key targeted drug option in multiple solid tumors.

In the latest CAPItello-291 study, capivasertib combined with fulvestrant significantly improved progression-free survival (PFS), especially in the genetically altered subgroup, PFS reached more than twice that of the control group. The patient's tumor shrinkage rate and disease stabilization time were significantly prolonged, and the efficacy was still stable for people who had become resistant to previous CDK4/6 inhibitors. This research result prompted its inclusion in the recommended sequence in international guidelines. Other trials, such as CAPItello-280 and CAPItello-204, have also shown that the drug has an observable objective response rate in ovarian cancer and other solid tumors, especially after multiple lines of treatment. It still maintains a certain anti-tumor activity, indicating that it still has clinical significance in a drug-resistant environment.

From the perspective of safety and overall use experience, capivasertib ’s tolerability is within a manageable range. Adverse reactions mainly include diarrhea, rash, hyperglycemia, fatigue, etc., which are related to its impact on the AKT pathway. Most side effects are controllable 1–2 and can be improved by adjusting the dosage, suspending the medication for a short period, and cooperating with symptomatic treatment. Special attention should be paid to the fact that some patients may experience blood sugar fluctuations, so metabolic indicators need to be monitored regularly during treatment. Taken together, with its precise targeting mechanism, significant clinical benefits for patients with genetic mutations, and manageable safety, capisete tablets have gradually become an important treatment option for advanced breast cancer and other AKT pathway-related tumors, and as more trials advance, its clinical status is expected to be further improved.

References:https://www.cancer.gov/publications/dictionaries/cancer-drug/def/capivasertib