Development

Merck posts first positive Phase III data for TROP2 ADC sacituzumab tirumotecan in endometrial cancer

Merck (NYSE: MRK) reported that sacituzumab tirumotecan endometrial cancer data from the Phase III TroFuse-005 trial met both co-primary endpoints of overall survival and progression-free survival versus chemotherapy, marking the first time a TROP2-directed antibody-drug conjugate has demonstrated a statistically significant survival benefit in this setting. The readout positions sac-TMT as a potential new standard of care for patients with advanced or recurrent endometrial cancer who have exhausted platinum-based chemotherapy and immunotherapy — a population with few established options.

Sac-TMT was developed by Kelun-Biotech (6990.HK), a subsidiary of Kelun Pharmaceutical (002422.SZ), and licensed to Merck for development in all territories outside of Greater China in a 2022 deal. The readout represents the first Phase III data to be reported by Merck for the program.

TroFuse-005 (NCT06132958) is a randomized, active-controlled, open-label, multicenter global Phase III trial evaluating sac-TMT against treatment of physician's choice (TPC) — consisting of doxorubicin or paclitaxel — in 776 patients with endometrial carcinoma and carcinosarcoma who had previously received platinum-based chemotherapy and anti-PD-1/PD-L1 immunotherapy, either together or separately.

At a pre-specified interim analysis, sac-TMT met both co-primary endpoints with statistically significant and, according to Merck, clinically meaningful improvements in OS and PFS by blinded independent central review versus TPC. The trial also reached its key secondary endpoint of objective response rate. Merck did not disclose specific numerical values — hazard ratios, median survival estimates, or response rates — in the press release; full data are expected to be presented at an upcoming medical meeting.

The safety profile was consistent with prior sac-TMT studies, with no new safety signals identified. Detailed adverse event data were not released.

The endometrial cancer treatment context

The TroFuse-005 readout arrives at a moment of rapid evolution in endometrial cancer treatment, but one that has left a specific patient population poorly served. First-line approvals for advanced or recurrent disease have accumulated quickly — Merck's own Keytruda (pembrolizumab) combined with carboplatin and paclitaxel, GSK's Jemperli (dostarlimab) plus chemotherapy, and AstraZeneca's durvalumab-based regimen have each secured regulatory clearance in the front-line setting over the past two years. These approvals, however, do not address patients who progress after both platinum-based chemotherapy and immunotherapy.

In that later-line setting, options are narrow. Eisai and Merck's Lenvima (lenvatinib) combined with pembrolizumab carries approval for pMMR/non-MSI-H endometrial carcinoma after prior systemic therapy, but its pivotal trial excluded carcinosarcoma and enrolled a population that was largely immunotherapy-naïve — limiting its applicability to patients who have already received a checkpoint inhibitor. Karyopharm's Xpovio (selinexor), an XPO1 nuclear export inhibitor, is approved in the post-platinum, post-immunotherapy setting and explicitly includes carcinosarcoma, but carries a meaningful tolerability burden including nausea, fatigue, and thrombocytopenia.

TroFuse-005 enrolled both endometrial carcinoma and carcinosarcoma patients, a design choice that, if reflected in the eventual label, would address a gap that lenvatinib plus pembrolizumab does not cover.

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TROP2 ADC competitive landscape

Sac-TMT is a TROP2-directed antibody-drug conjugate carrying a belotecan-derived topoisomerase I inhibitor payload. Its structural distinguishing feature is a bifunctional linker designed to maximize payload delivery to tumor cells while limiting systemic payload loss — a design Merck has characterized as unique among TROP2-directed ADCs currently in development.

The most direct comparator in the TROP2 ADC class is Gilead Sciences' Trodelvy (sacituzumab govitecan), the first approved TROP2-directed ADC, which holds US FDA approval in triple-negative breast cancer, HR+/HER2-negative breast cancer, and urothelial carcinoma. Sacituzumab govitecan has not secured approval in endometrial cancer, and no Phase III data in that indication have been reported. If sac-TMT reaches approval in endometrial cancer, it would occupy TROP2 ADC territory in a gynecologic tumor type where sacituzumab govitecan does not currently compete.

Cross-trial comparisons between sac-TMT and sacituzumab govitecan are limited by differences in patient populations, prior treatment histories, and trial designs, and no head-to-head data exist. The TroFuse-005 comparator arm — physician's choice of doxorubicin or paclitaxel — reflects the practical reality of the post-platinum, post-immunotherapy setting rather than a novel active comparator, which means the magnitude of benefit relative to more recently approved agents in adjacent settings cannot be directly assessed from this dataset.

Sac-TMT approval pathway and broader TroFuse program

TroFuse-005 represents the first positive Phase III readout from Merck's TroFuse clinical development program, which currently comprises 17 ongoing global Phase III trials across multiple tumor types. The program includes 10 trials in women's cancers and spans endometrial, bladder, breast, cervical, gastric, non-small cell lung, and ovarian cancer indications, evaluating sac-TMT as both monotherapy and in combination with immunotherapies. An ongoing trial, TroFuse-033, is evaluating sac-TMT in first-line mismatch repair-proficient endometrial cancer, extending the program into earlier disease settings.

Merck said the TroFuse-005 data will be presented at an upcoming medical meeting and discussed with regulatory authorities worldwide; no specific submission timeline or regulatory filing date was disclosed.


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