Tasfygo (tasurgratinib) / Eisai, SciClone - LARVOL DELTA

Results of a multicenter phase 2 basket trial evaluating the efficacy of tasurgratinib (E7090) in patients with advanced solid tumors with fibroblast growth factor receptor (FGFR) gene alteration, including those with primary brain tumors: FORTUNE study. (SNO 2025) - "Primary endpoint was met in Group B. Tasurgratinib demonstrated clinical activity in pts with selected FGFR-mutated tumors. Additional recruitment of pts has been resumed (jRCT2031210043)."

Clinical • Metastases • P2 data • Pan tumor • Biliary Cancer • Biliary Tract Cancer • Brain Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR • FGFR1 • FGFR2

Results of a multicenter phase 2 basket trial evaluating the efficacy of tasurgratinib (E7090) in patients with advanced solid tumors with fibroblast growth factor receptor (FGFR) gene alteration, including those with primary brain tumors: FORTUNE study. (WFNOS 2025) - "Primary endpoint was met in Group B. Tasurgratinib demonstrated clinical activity in pts with selected FGFR-mutated tumors. Additional recruitment of pts has been resumed (jRCT2031210043)."

Clinical • Metastases • P2 data • Pan tumor • Biliary Cancer • Biliary Tract Cancer • Brain Cancer • Cholangiocarcinoma • Solid Tumor • FGFR • FGFR1 • FGFR2

Sequential Fibroblast Growth Factor Receptor Inhibition in Intrahepatic Cholangiocarcinoma: Navigating an Evolving Landscape of Resistance and Opportunity-A Case Report and Current Opinion. (PubMed, Oncol Ther) - "Here, we report a case of FGFR2-rearranged iCCA where the patient achieved a radiographic partial response (PR) to tasurgratinib (a third-line FGFR inhibitor) following prior progression on pemigatinib and futibatinib. More broadly, this report serves as a basis for a current opinion on the evolving landscape of sequential FGFR inhibition in iCCA. We delve into the complexities of acquired resistance, dissect the arguments for and against prolonged FGFR pathway blockade, explore the impact of co-occurring genomic alterations, discuss the controversies, research priorities, and the urgent need for a balanced perspective to guide future clinical practice and trial design in this rapidly advancing but still uncertain field."

Journal • Biliary Cancer • Biliary Tract Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR • FGFR2

Tasurgratinib (E7090) for cholangiocarcinoma with fibroblast growth factor receptor 2 fusions/rearrangements: a multicenter, open-label, Phase 2 study. (PubMed, Jpn J Clin Oncol) - P2 | "The primary endpoint (ORR) met the study's predefined success criteria. Tasurgratinib had a manageable safety profile consistent with previous reports and the known pharmacological profile of FGFR inhibitors."

Journal • P2 data • Biliary Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR2

A Post-marketing Observational Study of Tasfygo in Participants With Unresectable Biliary Tract Cancer With Fibroblast Growth Factor Receptor 2 (FGFR2) Fusion Gene Positivity Who Progressed After Chemotherapy (clinicaltrials.gov) - P=N/A | N=60 | Recruiting | Sponsor: Eisai Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Biliary Cancer • Biliary Tract Cancer • Oncology • Solid Tumor

NCCH2006/MK010 Trial (FORTUNE Trial) (clinicaltrials.gov) - P2 | N=75 | Recruiting | Sponsor: National Cancer Center, Japan | Active, not recruiting ➔ Recruiting | N=46 ➔ 75 | Trial completion date: Dec 2024 ➔ Mar 2028 | Trial primary completion date: Dec 2024 ➔ Mar 2028

Enrollment change • Enrollment open • Trial completion date • Trial primary completion date • Solid Tumor • ALK • BRAF • EGFR • FGFR2 • FGFR4 • KRAS • NRAS • NTRK • ROS1

First Successful Treatment of Advanced Intrahepatic Cholangiocarcinoma with Tasurgratinib Following Regulatory Approval: A Case Report from Clinical Practice. (PubMed, Int J Mol Sci) - "We report the case of a 55-year-old female with advanced iCCA harboring an FGFR2-BICC1 fusion, who experienced a rapid clinical response to tasurgratinib following disease progression on gemcitabine, cisplatin, and durvalumab (GCD). This is the first report to describe the real-world clinical efficacy of tasurgratinib in an iCCA patient with FGFR2-BICC1 fusion. Our findings suggest that tasurgratinib can provide a rapid and durable response with manageable toxicity in molecularly selected patients who have progressed on standard therapies."

Journal • Anorexia • Biliary Cancer • Biliary Tract Cancer • Cholangiocarcinoma • Metabolic Disorders • Nephrology • Oncology • Renal Disease • Solid Tumor • BICC1 • FGFR2

A phase II basket trial evaluating the efficacy of tasurgratinib (E7090) in patients with advanced solid tumors with fibroblast growth factor receptor (FGFR) gene alteration: FORTUNE study. (ASCO 2025) - P2 | "In Group B, the primary endpoint was met. Tasurgratinib demonstrated clinical activity in pts with selected FGFR-mutated tumors. Further study is needed to validate these findings."

Clinical • Metastases • P2 data • Pan tumor • Biliary Cancer • Biliary Tract Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR • FGFR2

Effect of Tasurgratinib as an Orally Available FGFR1-3 Inhibitor on Resistance to a CDK4/6 Inhibitor and Endocrine Therapy in ER+/HER2- Breast Cancer Preclinical Models. (PubMed, Cancers (Basel)) - "FGF signaling plays a role in resistance to CDK4/6 inhibitors and ET in ER+ BC. Tasurgratinib has the potential to exhibit significant antitumor activity in combination with ET against ER+ BC via FGF signaling inhibition. These findings indicate the therapeutic potential of tasurgratinib in treating ER+ BC."

Journal • Preclinical • Breast Cancer • Endocrine Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ER • FGF10 • FGF2 • FGFR1 • HER-2

A Post-marketing Observational Study of Tasfygo in Participants With Unresectable Biliary Tract Cancer With Fibroblast Growth Factor Receptor 2 (FGFR2) Fusion Gene Positivity Who Progressed After Chemotherapy (clinicaltrials.gov) - P=N/A | N=60 | Not yet recruiting | Sponsor: Eisai Co., Ltd. | Trial completion date: Nov 2033 ➔ Nov 2030 | Initiation date: Feb 2025 ➔ Aug 2025 | Trial primary completion date: Nov 2032 ➔ Nov 2030

Trial completion date • Trial initiation date • Trial primary completion date • Biliary Cancer • Biliary Tract Cancer • Oncology • Solid Tumor

Tasurgratinib Succinate: First Approval. (PubMed, Drugs) - "The approval was based on the positive results of an open-label, single-arm, multicenter, phase II study conducted in Japan and China. This article summarizes the milestones in the development of tasurgratinib succinate leading to this first approval for biliary tract cancer."

Journal • Review • Biliary Cancer • Biliary Tract Cancer • Breast Cancer • Cholangiocarcinoma • Hepatology • Oncology • Solid Tumor • FGFR2

Eisai Enters into License Agreement for the Development and Distribution of Fibroblast Growth Factor (FGF) Receptor Selective Tyrosine Kinase Inhibitor Tasurgratinib in Greater China Region (Mainland China, Hong Kong, Macau, and Taiwan) with SciClone (Eisai Press Release) - "Eisai...announced today that the company has entered into a license agreement granting the exclusive development and distribution rights for the fibroblast growth factor (FGF) receptor selective tyrosine kinase inhibitor tasurgratinib succinate...in the Greater China region (mainland China, Hong Kong, Macau, and Taiwan, 'licensed regions') to a subsidiary of SciClone Pharmaceuticals (Holdings) Limited (Headquarters: Shanghai, China, 'SciClone'). Eisai will maintain the rights to tasurgratinib worldwide outside of the licensed regions and continue to manufacture and market it in Japan, where it has been already launched. Under the terms of this agreement, Eisai will receive a contractual upfront payment. Additionally, Eisai will receive milestone payments based on the progress of development and regulatory approval, as well as sales milestone payments and certain royalties based on sales revenue after the product launch."

Licensing / partnership • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

A Post-marketing Observational Study of Tasfygo in Participants With Unresectable Biliary Tract Cancer With Fibroblast Growth Factor Receptor 2 (FGFR2) Fusion Gene Positivity Who Progressed After Chemotherapy (clinicaltrials.gov) - P=N/A | N=60 | Not yet recruiting | Sponsor: Eisai Co., Ltd.

New trial • Biliary Cancer • Biliary Tract Cancer • Oncology • Solid Tumor

PMDA regulatory update on approval and revision of the precautions for use of anticancer drugs; approval of sacituzumab govitecan for breast cancer, fruquintinib for colorectal cancer, amivantamab for lung cancer, repotrectinib for lung cancer, tasurgratinib for biliary tract cancer, enfortumab vedotin plus pembrolizumab for urothelial cancer, and dabrafenib plus trametinib for glioma in Japan. (PubMed, Int J Clin Oncol) - No abstract available

Japanese regulatory • Journal • Biliary Cancer • Biliary Tract Cancer • Brain Cancer • Breast Cancer • CNS Tumor • Colorectal Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Glioma • Lung Cancer • Oncology • Solid Tumor • Urothelial Cancer

Potential predictive biomarkers for a fibroblast growth factor receptor (FGFR) inhibitor: Phase 1b trial of tasurgratinib (E7090) with endocrine therapies (ET) for ER+, HER2+ recurrent/metastatic breast cancer (BC) resistant to CDK4/6 inhibitors (SABCS 2024) - P1 | "Part 1 included treatment with fulvestrant (FUL) 500 mg + E7090 (105 or 140 mg) or exemestane (EXE) 25 mg + E7090 (105 or 140 mg). These results emphasize that FGFR pathway activation evaluated with mRNA expression of selected genes at BL—rather than FGFR gene abnormalities—is a key molecular determinant for sensitivity to E7090, an FGFR inhibitor. Future validation of these biomarkers is necessary in a larger population of people with ER+/HER2− BC."

Biomarker • Metastases • P1 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • CCND1 • ER • FGF19 • FGF3 • FGF4 • FGFR • FGFR1 • HER-2 • PIK3CA • TP53

A Study of E7090 as Monotherapy and in Combination With Other Anticancer Agents in Participants With Estrogen Receptor Positive (ER+) and Human Epidermal Growth Receptor 2 Negative (HER2-) Recurrent/Metastatic Breast Cancer (clinicaltrials.gov) - P1 | N=72 | Active, not recruiting | Sponsor: Eisai Co., Ltd. | Trial completion date: Dec 2024 ➔ Mar 2026 | Trial primary completion date: Dec 2024 ➔ Mar 2026

Combination therapy • Metastases • Monotherapy • Trial completion date • Trial primary completion date • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER • FGFR • HER-2

A Study of E7090 in Participants With Unresectable Advanced or Metastatic Cholangiocarcinoma With Fibroblast Growth Factor Receptor (FGFR) 2 Gene Fusion (clinicaltrials.gov) - P2 | N=63 | Active, not recruiting | Sponsor: Eisai Co., Ltd. | Trial completion date: Sep 2024 ➔ Mar 2026 | Trial primary completion date: Sep 2024 ➔ Mar 2026

Metastases • Trial completion date • Trial primary completion date • Biliary Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR2

Study to Evaluate the Pharmacokinetics (PK) of E7090 (Herein Referred to as Tasurgratinib) and Its Metabolite in Participants With Mild and Moderate Hepatic Impairment Compared to Healthy Participants (clinicaltrials.gov) - P1 | N=18 | Recruiting | Sponsor: Eisai Co., Ltd. | Trial completion date: Nov 2024 ➔ Nov 2026 | Trial primary completion date: Nov 2024 ➔ Nov 2026

Trial completion date • Trial primary completion date • Hepatology

ANTICANCER AGENT “TASFYGO TABLETS 35mg” (TASURGRATINIB SUCCINATE) LAUNCHED IN JAPAN FOR BILIARY TRACT CANCER WITH FGFR2 GENE FUSION OR REARRANGEMENTS (Eisai Press Release) - "Eisai...announced today that it has launched fibroblast growth factor receptor (FGFR) selective tyrosine kinase inhibitor 'TASFYGO Tablets 35mg' (generic name: tasurgratinib succinate) in Japan for the treatment of patients with unresectable biliary tract cancer with FGFR2 gene fusions or rearrangements that progressed after cancer chemotherapy. The product received manufacturing and marketing approval in Japan on September 24, 2024, and was published in Japan’s National Health Insurance Drug Price List today....The approval of TASFYGO in Japan is based on data such as the results of a multicenter, open-label, single arm clinical phase II trial (Study 201) conducted by Eisai in Japan and China."

Launch Japan • Biliary Tract Cancer

Tasurgratinib in patients with cholangiocarcinoma or gastric cancer: Expansion part of the first-in-human phase I study. (PubMed, Cancer Sci) - "Five partial responses (83.3%) in cholangiocarcinoma patients and one partial response (11.1%) in gastric cancer patients were observed; median progression-free survival was 8.26 months (95% confidence interval [CI] 3.84, not evaluable [NE]) and 3.25 months (95% CI 0.95, 4.86), and overall survival was 22.49 months (95% CI 6.37, NE) and 4.27 months (95% CI 2.23, 7.95), respectively, in the two groups. In conclusion, Tasurgratinib 140 mg has a tolerable safety profile with good clinical efficacy in patients with cholangiocarcinoma harboring FGFR2 gene rearrangements."

Journal • P1 data • Biliary Cancer • Cholangiocarcinoma • Dermatology • Gastric Cancer • Gastrointestinal Cancer • Metabolic Disorders • Nephrology • Oncology • Renal Disease • Solid Tumor • FGF23 • FGFR2

Effect of tasurgratinib as an orally available FGFR1-3 inhibitor on resistance to a CDK4/6 inhibitor and endocrine therapy in ER(+)/HER2(-) breast cancer preclinical models (EORTC-NCI-AACR 2024) - P1 | "Palbociclib (PAL) was administered orally daily at 100 mg/kg. Fulvestrant (FUL) was administered subcutaneously weekly at 250 mg/kg or 5 mg/mouse. Elacestrant (ELA) was administered orally daily at 30 mg/kg in the ESR1-mutant BC PDX model studies because it is known to be effective also in case of ESR1-mutant... These data suggest that activation of FGFR signaling has a role in resistance to CDK4/6 inhibitor and ET in ER(+) BC. Furthermore, tasurgratinib has a potential to exhibit significant antitumor activity in combination with ET against ER(+) BC based on inhibition of FGFR signaling pathway. Phase 1 study as a monotherapy or in combination with FUL or exemestane for ER(+)/HER2(-) BC patients (NCT04572295) is currently under evaluation."

Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • ER • FGF10 • FGF2 • FGFR1 • HER-2

ANTICANCER AGENT 'TASFYGO TABLETS 35mg' (TASURGRATINIB SUCCINATE) APPROVED IN JAPAN FOR BILIARY TRACT CANCER WITH FGFR2 GENE FUSIONS OR REARRANGEMENTS (Eisai Press Release) - "Eisai Co., Ltd... announced today that it has obtained manufacturing and marketing approval for fibroblast growth factor receptor (FGFR) selective tyrosine kinase inhibitor 'TASFYGO Tablets 35mg' (tasurgratinib succinate) in Japan for the treatment of patients with unresectable biliary tract cancer with FGFR2 gene fusions or rearrangements that progressed after cancer chemotherapy. In Japan, it has received orphan drug designation from the Ministry of Health, Labour and Welfare (MHLW), and the marketing authorization application was submitted in December 2023....This approval is based on data such as the results of a multicenter, open-label, single-arm clinical phase II trial (Study 201) conducted by Eisai in Japan and China."

Japan approval • Biliary Tract Cancer • Cholangiocarcinoma

Phase Ib trial of tasurgratinib (E7090) with or without endocrine therapies for patients (pts) with ER+, HER2− recurrent/metastatic breast cancer (BC) after receiving a CDK4/6 inhibitor. (ASCO 2024) - P1 | "In part 1, pts were treated with fulvestrant (FUL) 500 mg + E7090 (105 mg [Cohort 1] or 140 mg [Cohort 2]), or exemestane 25 mg + E7090 (105 mg [Cohort 3] or 140 mg [Cohort 4]). E7090 + FUL had a manageable safety profile. The combination showed promising preliminary antitumor activity in ER+ HER2− BC previously treated with a CDK4/6i; its ORR was 21.9%. Our results support the further development of this combination for HR+/HER2− advanced BC after a CDK4/6i."

Clinical • Metastases • P1 data • Breast Cancer • Cardiovascular • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hypertension • Metabolic Disorders • Nephrology • Oncology • Renal Disease • Retinal Disorders • Solid Tumor • CDK4 • ER • HER-2

EISAI SHOWCASES ONCOLOGY PORTFOLIO AND PIPELINE AT ASCO 2024 (Eisai Press Release) - "Additional pipeline research to be presented in poster sessions include an overview of a Phase 2 study of BB-1701, an antibody drug conjugate targeting HER2, in previously treated patients with HER2-positive or HER2-low unresectable or metastatic breast cancer (NCT06188559; Abstract #TPS1122), findings from a Phase 1b trial of tasurgratinib (development code: E7090) with or without endocrine therapies for patients with ER-positive, HER2−negative recurrent/metastatic breast cancer after receiving a CDK4/6 inhibitor (NCT04572295; Abstract #3103), as well as the dose-expansion part of a Phase 1b global study of E7386 in combination with lenvatinib in patients with hepatocellular carcinoma and other solid tumors including endometrial cancer (NCT04008797; Abstract #TPS3169)."

P1 data • Trial status • Endometrial Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer

Study to Evaluate the Pharmacokinetics (PK) of E7090 (Herein Referred to as Tasurgratinib) and Its Metabolite in Participants With Mild and Moderate Hepatic Impairment Compared to Healthy Participants (clinicaltrials.gov) - P1 | N=18 | Recruiting | Sponsor: Eisai Co., Ltd. | Trial completion date: Aug 2024 ➔ Nov 2024 | Trial primary completion date: Aug 2024 ➔ Nov 2024

Trial completion date • Trial primary completion date • Hepatology