FDA Approves LONSURF (trifluridine/tipiracil) in Combination With Bevacizumab for Adult Patients With Metastatic Colorectal Cancer (mCRC)

Taiho Oncology, Inc. and Taiho Pharmaceutical Co., Ltd. announced that the U.S. Food and Drug Administration (FDA) has approved LONSURF (trifluridine/tipiracil) as a single agent or in combination with bevacizumab for the treatment of adult patients with metastatic colorectal cancer (mCRC) previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy.

“The FDA approval of this combination provides patients with mCRC an important new treatment option, one that has been shown to extend life in addition to other benefits and which I believe will change the treatment landscape for this patient population,” said Marwan Fakih, MD, Professor, Medical Oncology and Therapeutics Research, City of Hope, Duarte, Calif., and lead U.S. investigator for the pivotal Phase 3 SUNLIGHT trial that evaluated this combination. “Notably, the use of LONSURF plus bevacizumab in these patients did not result in an increase in potentially intolerable side effects that might limit the utility of this combination.”

The results from the Phase 3 SUNLIGHT trial, which were published in the New England Journal of Medicine in May 2023, demonstrated that the combination of LONSURF plus bevacizumab provided statistically significant and clinically meaningful improvements in overall survival (OS) and progression-free survival (PFS) for patients with mCRC following disease progression or intolerance on two prior chemotherapy regimens compared to LONSURF alone. This was the first Phase 3 study against an active control in third-line mCRC that demonstrated statistically significant efficacy and safety. Key results include:

  • Median OS was 10.8 months in the LONSURF plus bevacizumab arm versus 7.5 months in the LONSURF arm (hazard ratio [HR]: 0.61, 95% confidence interval [CI]: 0.49-0.77, p<0.001). This improvement in OS represented a 39% reduction in the risk of death in patients with mCRC.
  • The median PFS was 5.6 months in the LONSURF plus bevacizumab arm versus 2.4 months in the LONSURF arm (HR: 0.44, 95% CI: 0.36-0.54, p<0.001), indicating a 56% relative risk reduction of disease progression.1
  • Results were consistent across subgroups regardless of age, sex, location of primary disease, number of metastatic sites, KRAS mutation status, and prior bevacizumab treatment.
  • Median time to worsening of the ECOG performance status score from 0 or 1 to 2 or more was 9.3 months (95% CI: 8.3-10.6) in the LONSURF plus bevacizumab arm versus 6.3 months (95% CI: 5.6-7.2) in the LONSURF arm (HR: 0.54, 95% CI: 0.43-0.67).
  • The OS and PFS benefits of LONSURF plus bevacizumab were associated with maintenance of quality of life from baseline to cycle 6 and no clinically relevant changes in mean scores were observed in any subdomains for EORTC QLQ-C30 and EuroQol EQ-5D-5L health-related quality of life questionnaires.
  • The combination of LONSURF plus bevacizumab had a manageable safety profile as was expected based on the known profile of each agent. The most frequent severe treatment emergent adverse events for LONSURF plus bevacizumab versus LONSURF alone were neutropenia (43.1% vs 32.1%) and anemia (6.1% vs 11.0%), respectively.

“The treatment of advanced colorectal cancer has been a core focus of our work at Taiho Oncology since our inception and with good reason: approximately 22% of patients with colorectal cancer in the U.S. are diagnosed after the cancer has metastasized,” said Timothy Whitten, President and Chief Executive Officer, Taiho Oncology, Inc. “The FDA approval of LONSURF in combination with bevacizumab is another example of how we are continuing to advance care in this disease and provide new hope to patients and their families.”

In 2023, the National Comprehensive Cancer Network (NCCN) Drugs and Biologics Compendium (NCCN Compendium) for Colon Cancer and Rectal Cancer was updated to include a Category 2A recommendation for trifluridine/tipiracil as subsequent therapy, either single agent or in combination with bevacizumab (preferred) (per NCCN, an FDA-approved biosimilar is an appropriate substitute for bevacizumab), as treatment options for patients who have progressed through all available regimens besides regorafenib or trifluridine/tipiracil with or without bevacizumab.

“From Taiho Pharmaceutical’s initial discovery of LONSURF to this latest regulatory milestone, we are appreciative of the investigators and patients who helped to contribute to our growing body of knowledge of this important therapeutic through their participation in our clinical development programs,” said Fabio Benedetti, MD, Global Chief Medical Officer for Oncology, Taiho Pharmaceutical Co., Ltd. “And now we look forward to supporting healthcare professionals in the treatment of patients with mCRC who may be candidates for treatment with LONSURF in combination with bevacizumab.”

On July 31, 2023, Servier, which conducted the SUNLIGHT trial with Taiho Oncology, received approval from the European Commission for LONSURF in combination with bevacizumab for the treatment of adult patients with mCRC who have received two prior anti-cancer treatment regimens, including fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapies, anti-VEGF agents, and/or anti-EGFR agents. The Marketing Authorization covers the 27 countries of the European Union as well as IcelandNorthern IrelandLiechtenstein and Norway.

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