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Gedatolisib (gedatolisib)
Gedatolisib will be administered once weekly on the first day for each of the four weeks during the
Gedatolisib is a dual PI3K/mTOR inhibitor approved for treatment of hormone receptor-positive breast cancer. It works by blocking two key proteins that promote cancer cell growth and survival. This dual-targeting approach offers potential advantages over single-pathway inhibitors in overcoming resistance mechanisms.
At a glance
| Generic name | gedatolisib |
|---|---|
| Sponsor | Pfizer Inc. |
| Drug class | Gedatolisib will be administered once weekly on the first day for each of the four weeks during the |
| Therapeutic area | Oncology |
| Phase | discontinued |
Mechanism of action
Gedatolisib works by targeting two closely related proteins called PI3K and mTOR that act like master switches controlling cancer cell growth. These proteins normally help cells receive signals to divide and survive, but cancer cells often exploit this system to grow uncontrollably. By blocking both proteins simultaneously, Gedatolisib shuts down multiple growth pathways at once, making it harder for cancer cells to adapt and become resistant to treatment. The advantage of targeting both proteins together is that cancer cells have fewer escape routes. If a tumor cell manages to work around a block on just one protein, it often becomes more dependent on the other, which is then shut down by Gedatolisib. This dual approach is particularly useful in hormone receptor-positive breast cancers, which frequently have mutations that activate the PI3K/mTOR pathway. By attacking both targets, Gedatolisib can help prevent the resistance that sometimes develops when these cancer types are treated with single-target drugs. In clinical practice, Gedatolisib is used as part of combination therapy with other cancer treatments like hormone therapy. This combination approach takes advantage of different mechanisms—Gedatolisib disrupts growth signals while other drugs block hormone receptors—to attack cancer cells from multiple angles and improve treatment effectiveness.
Approved indications
Pipeline indications
- Lung Cancer Squamous Cell — discontinued
Common side effects
Key clinical trials
- Gedatolisib, Hydroxychloroquine or the Combination for Prevention of Recurrent Breast Cancer ("GLACI (Phase 1/2)
- Study of Paclitaxel, Carboplatin, and PF-05212384 in Advanced or Metastatic NSCLC (UF-STO-LUNG-002) (Phase 1/2)
- A Study Of PF-05212384 Plus Irinotecan Vs Cetuximab Plus Irinotecan In Patients With KRAS And NRAS W (Phase 2)
- A Study Of PF-05212384 In Combination With Other Anti-Tumor Agents and in Combination With Cisplatin (Phase 1)
- Gedatolisib Plus Talazoparib in Advanced Triple Negative or BRCA1/2 Positive, HER2 Negative Breast C (Phase 1/2)
- A Study Of PF-05212384 Plus FOLFIRI Versus Bevacizumab Plus FOLFIRI In Metastatic Colorectal Cancer (Phase 1/2)
- Study of PF-05212384 (Also Known as PKI-587)Administered Intravenously To Subjects With Solid Tumors (Phase 1)
- Investigation Of The Metabolism, And Excretion Of [14c]-PF-05212384 In Healthy Male Volunteers (Phase 1)
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 |