Phase 1active not recruiting

Gedatolisib for Advanced triple-negative breast cancer (TNBC) and BRCA1/2-positive, HER2-negative breast cancer

Kari Wisinski

Reviewed by Blane Jackson, DDS, MBA. Educational analysis only. Read the editorial policy and disclosures.

NCT03911973 on ClinicalTrials.gov →

Study type

interventional

Design

Single-group, open-label, phas…

Target enrollment

37

Est. completion

2024-07

Investor scorecard

Probability of success

moderate

Timeline to catalyst

Data readout expected around mid-2024 (completion date July 2024).

Potential stock impact

Moderate

The combination has a strong biological rationale and talazoparib is already approved, but the trial is small and lacks a control arm. Early-phase data for gedatolisib have shown some activity, but PI3K inhibitors have been disappointing in TNBC. The primary endpoint of ORR will need to be high (likely >30%) to be considered promising. Given the challenges of treating TNBC and potential toxicity, the probability of success is moderate.


What is being tested?

This trial is testing a combination of two drugs for patients with advanced breast cancer that is either triple-negative or has BRCA1/2 mutations and is HER2-negative. Triple-negative breast cancer lacks receptors for estrogen, progesterone, and HER2, making it harder to treat. BRCA mutations impair DNA repair, making cancer cells vulnerable to certain drugs. The two drugs are gedatolisib, which blocks a protein called PI3K/mTOR that helps cancer cells grow, and talazoparib, a PARP inhibitor that prevents cancer cells from repairing their DNA. By combining them, the hope is to attack cancer cells in two ways at once, potentially making the treatment more effective than either drug alone.

How does the trial work?

The trial has two parts. In the first part (phase 1), a small group of patients receives increasing doses of talazoparib along with a fixed dose of gedatolisib to find the highest dose that doesn't cause severe side effects. This is called a safety run-in. Once the recommended dose is found, the second part (phase 2) enrolls more patients to receive that dose. All patients receive the combination treatment; there is no placebo or comparison group. Patients are treated until their cancer progresses or they experience unacceptable side effects. The trial is currently active but no longer recruiting, meaning all planned patients have been enrolled. The study is expected to be completed by July 2024.

What does success look like?

Success in the phase 1 part is finding a safe and tolerable dose. In the phase 2 part, the main measure of success is the objective response rate (ORR) - the percentage of patients whose tumors shrink significantly or disappear. For this trial, a meaningful ORR would likely be above 30-40%, based on historical data for similar treatments in this tough-to-treat population. Secondary measures include how long the response lasts, the clinical benefit rate at 16 weeks (which includes stable disease), and overall survival. If the ORR is high and responses are durable, it would suggest the combination is promising and warrant further study.

What it means for investors

For investors, this trial is important because it tests a novel combination that could address a high unmet need in triple-negative breast cancer and BRCA-mutated tumors. If the results are positive, it could boost the prospects for gedatolisib, which is being developed by Pfizer (though this trial is investigator-initiated). A positive outcome could lead to larger trials and eventual approval, potentially expanding the market for gedatolisib. However, the trial is small (37 patients) and lacks a control group, so results must be interpreted cautiously. If the ORR is high and safety is manageable, it could increase the probability of success for gedatolisib in this indication, positively impacting Pfizer's pipeline. Conversely, if the trial fails or shows modest efficacy, it could dampen enthusiasm. Investors should watch for data readouts, expected around mid-2024, and compare results with competing PARP inhibitors and PI3K inhibitors.


Trial endpoints

Primary endpoints

Maximum tolerated dose of talazoparib when combined with gedatolisib (phase 1 part)
Objective response rate (ORR) - percentage of patients whose tumors shrink or disappear (phase 2 part)

Secondary endpoints

Duration of response - how long tumor shrinkage lasts
Clinical benefit rate at 16 weeks - percentage of patients with tumor shrinkage or stable disease for at least 16 weeks
Overall survival - how long patients live from start of treatment
Rates of adverse events - safety profile

Competitive landscape

Triple-negative breast cancer (TNBC) accounts for about 15% of all breast cancers and has a poor prognosis, especially in advanced stages. BRCA-mutated HER2-negative breast cancers also represent a significant subset. The market for treatments in these indications is substantial, with PARP inhibitors already generating billions in sales. However, there is still a need for more effective therapies, especially for patients who progress on PARP inhibitors or who have TNBC without BRCA mutations. If this combination proves effective, it could capture a share of this market, but it will face competition from established drugs and emerging combinations.

DrugSponsorPhaseDifferentiation
OlaparibAstraZeneca/MerckPhase 1PARP inhibitor approved for BRCA-mutated HER2-negative breast cancer; not combined with PI3K inhibitor.
TalazoparibPfizerPhase 1PARP inhibitor approved for BRCA-mutated HER2-negative breast cancer; being tested here in combination with gedatolisib.
AlpelisibNovartisPhase 1PI3K inhibitor approved for HR+/HER2- breast cancer with PIK3CA mutations; not for TNBC.
Sacituzumab govitecanGileadPhase 1Antibody-drug conjugate for TNBC; different mechanism (targets Trop-2).

Historical context

Prior trial results

Gedatolisib has been studied in earlier phase trials for solid tumors, showing manageable safety and some antitumor activity. Talazoparib is already approved for BRCA-mutated HER2-negative breast cancer based on the EMBRACA trial, which showed improved progression-free survival compared to chemotherapy. However, the combination of gedatolisib and talazoparib is novel, and no prior results are available for this specific combination.

Regulatory history

Talazoparib received FDA approval in 2018 for BRCA-mutated HER2-negative breast cancer. Gedatolisib is not yet approved for any indication. This trial is investigator-initiated and not part of a formal registration program, so it may not directly lead to approval but could inform future development.

Similar drug precedents

Other PI3K inhibitors like alpelisib have shown benefit in HR+ breast cancer but have limited activity in TNBC. PARP inhibitors have shown activity in BRCA-mutated breast cancer, but resistance develops. Combining a PI3K inhibitor with a PARP inhibitor is a rational strategy to overcome resistance, as preclinical studies suggest synergy. However, similar combinations have faced toxicity challenges, so safety will be a key factor.

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