Fruzaqla (fruquintinib) / Eli Lilly, Hutchmed, Takeda - LARVOL DELTA

In-silico analysis of potential phytochemicals targeting mitogen activating protein kinase-14 (MAPK14) gene in colorectal cancer. (PubMed, Sci Rep) - "We also included Fruquintinib, an FDA-approved anticancer drug, as a reference compound for molecular docking with MAPK14. Compounds meeting acceptable ADMET profiles were further analyzed using molecular docking, DFT, and MD simulations to identify potential MAPK14 inhibitors. Compound 1 (CID: 44586092) was discovered in our investigation to be a potential therapy for CRC associated with MAPK14."

Journal • Colorectal Cancer • Oncology • Solid Tumor • MAPK14

A novel imaging biomarker, quantitative vessel tortuosity, captures the antiangiogenic effect of fruquintinib in metastatic colorectal cancer (ESMO-GI 2025) - P3 | "Fruquintinib prevented the formation of heterogeneous vasculature within 6 weeks, shown by significant reduction in QVT features compared with P, suggesting a causal association with its MOA as an angiogenic inhibitor. Future analyses are planned to include liver lesions and develop a predictive biomarker of survival using QVT."

Biomarker • Metastases • Colorectal Cancer • Oncology • Solid Tumor

Efficacy and safety of fruquintinib vs placebo by metastatic site in metastatic colorectal cancer: A FRESCO-2 subgroup analysis (ESMO-GI 2025) - P3 | "This analysis suggests that fruquintinib may be an effective and tolerable treatment option for pts with mCRC who have liver only, bone, or peritoneal mets at BL."

Clinical • Metastases • Colorectal Cancer • Oncology • Solid Tumor

Real-world data from fruquintinib in later line metastatic colorectal cancer (ESMO-GI 2025) - "Its use was studied in the FRESCO 2 trial, after 2 lines of therapy plus prior progression on/ intolerance to trifluridine/tipiracil (FTD/TPI) and/or regorafenib...Med number of previous treatment lines was 3 [2-7]; of note, 20 patients (86.7%) were previously treated with the combination FTD/TPI + Bevacizumab (B), whilst only 2 with FTD/FPI... To our knowledge, this is one of the first non-Asian fruquintinib datasets, and one of the first analyzing sequencing results from FTD/TPI + B followed by fruquintinib. Despite the small sample size and very short follow up, we observed a manageable safety profile and an efficacy trend, despite modest outcomes, picturing a highly refractory disease setting and a possible role of previous treatments on VEGFR targeting. We intend to broaden our accrual and increase follow up time to evaluate safety and more mature outcomes."

Clinical • Metastases • Real-world • Real-world evidence • Colorectal Cancer • Oncology • Solid Tumor • FLT1

Phase II Trial of 5-Fluorouracil (5FU)-Based Therapy in Combination With Fruquintinib in Patients With Locally Advanced Unresectable or Metastatic Colorectal Cancer (clinicaltrials.gov) - P2 | N=50 | Not yet recruiting | Sponsor: The Methodist Hospital Research Institute

New P2 trial • Colorectal Cancer • Oncology • Solid Tumor

A Study to Monitor the Fruzaqla Treatment of Adults With Metastatic Colorectal Cancer (mCRC) in South Korea (clinicaltrials.gov) - P=N/A | N=600 | Not yet recruiting | Sponsor: Takeda

New trial • Colorectal Cancer • Oncology • Solid Tumor

Redefining the Use of Regorafenib and Trifluridine/Tipiracil Without Bevacizumab in Refractory Metastatic Colorectal Cancer: Findings from the ReTrITA Study. (PubMed, Cancers (Basel)) - "Background: Regorafenib (R) and trifluridine/tipiracil (T) are approved treatments for metastatic colorectal cancer (mCRC) in refractory cases. ReTrITA confirms the efficacy of R and T as monotherapies and provides compelling real-world evidence that the R/T sequence improves survival in refractory mCRC. These findings support a regorafenib-first approach in patients who are eligible, and they emphasise the need for future research into combination strategies and comparisons with newer drugs such as fruquintinib."

Journal • Colorectal Cancer • Hematological Disorders • Neutropenia • Oncology • Solid Tumor

A phase II study to evaluate the efficacy and safety of fruquintinib combined with envafolimab in patients with advanced or unresectable locally advanced osteosarcoma and soft tissue sarcoma. (ASCO 2025) - P2 | "6 pts had previously received VEGF TKIs including 5 with anlotinib and 1 with pazopanib... The combination of fruquintinib with envafolimab was well tolerated and demonstrated preliminary clinical activity in advanced or locally advanced OS and STS who had failed to first-line chemotherapy. Enrollment is ongoing and updated data will be presented in the future."

Clinical • Metastases • P2 data • Dyslipidemia • Hypertriglyceridemia • Oncology • Osteosarcoma • Renal Disease • Sarcoma • Soft Tissue Sarcoma • Solid Tumor • Synovial Sarcoma

Digoxin Combined With Fruquintinib and Tislelizumab in Microsatellite Stabilized Metastatic Colorectal Cancer Patients (clinicaltrials.gov) - P1/2 | N=20 | Not yet recruiting | Sponsor: Fudan University

New P1/2 trial • Tumor mutational burden • Colorectal Cancer • Oncology • Solid Tumor • PD-L1

Renal-Limited Thrombotic Microangiopathy Induced by Fruquintinib and Tislelizumab: A Case Report. (PubMed, Nephrology (Carlton)) - "Early detection through renal biopsy and prompt withdrawal of the causative agents may prevent irreversible renal damage. Further research is required to better understand the pathophysiology of TMA in this context and to inform management strategies."

Journal • Cardiovascular • Colorectal Cancer • Focal Segmental Glomerulosclerosis • Glomerulonephritis • Hypertension • Nephrology • Oncology • Rectal Cancer • Renal Disease • Solid Tumor

Takeda launches Fruzaqla in Korea for hard-to-treat colorectal cancer (Korea Biomedical Review) - "Takeda Korea has launched Fruzaqla (fruquintinib), a once-daily oral treatment for metastatic colorectal cancer (mCRC), making it the first VEGFR-1, -2, and -3 selective inhibitor approved in the country. Cleared by the Ministry of Food and Drug Safety (MFDS) in March under Korea’s Global Innovative Product on Fast Track (GIFT) system, Fruzaqla is indicated for patients who have failed at least three prior treatments, including fluoropyrimidine-, oxaliplatin- and irinotecan-based chemo, anti-VEGF or anti-EGFR agents, and either trifluridine/tipiracil or regorafenib....Backed by data from the global phase 3 FRESCO-2 trial, Fruzaqla cut the risk of death by 34 percent versus placebo, extending median overall survival to 7.4 months from 4.8 months."

Launch non-US • Colorectal Cancer

The efficacy and safety of regorafenib/fruquintinib combined with PD-1/PD-L1 for metastatic colorectal cancer: a meta-analysis based on single-arm studies. (PubMed, Front Immunol) - "These findings offer new insights for treating mCRC, although they should be validated through large randomized controlled trials. https://www.crd.york.ac.uk/PROSPERO, identifier CRD42024582268."

Clinical • Journal • Retrospective data • Review • Colorectal Cancer • Oncology • Solid Tumor • PD-1 • PD-L1

Vitamin E Combined With Fruquintinib and Tislelizumab in Microsatellite Stabilized Metastatic Colorectal Cancer Patients (clinicaltrials.gov) - P2 | N=25 | Recruiting | Sponsor: Fudan University | Not yet recruiting ➔ Recruiting | Trial primary completion date: Feb 2025 ➔ Dec 2025

Enrollment open • Trial primary completion date • Tumor mutational burden • Colorectal Cancer • Oncology • Solid Tumor • BRAF • KRAS • MSI • PD-L1

Safety of fruquintinib in young and late-elderly Chinese patients with colorectal cancer in real-world clinical practice: Age subgroup analysis of a fruquintinib phase IV study. (ASCO 2025) - P=N/A | "The safety profile of fruquintinib was comparable across the two age subgroups, with younger CRC patients receiving more intensive treatment. The duration of combination therapy with fruquintinib was longer than with fruquintinib alone, which may potentially lead to improved survival in both subgroups."

Clinical • P4 data • Real-world • Real-world evidence • Colorectal Cancer • Dermatology • Dysphonia • Fatigue • Hypertension • Oncology • Solid Tumor

Real-world evidence of fruquintinib (Fruq) efficacy after regorafenib (Rego) and trifluridine–tipiracil (TAS-102) in refractory metastatic colorectal cancer (mCRC). (ASCO 2025) - " This retrospective, multi-site cohort study evaluated outcomes in 33 mCRC pts who received Fruq following treatment with Rego and/or TAS-102 with or without bevacizumab. This real-world analysis highlights the clinical benefit of Fruquintinib in mCRC patients following treatment with Regorafenib and/or TAS-102. The data suggest flexibility in treatment choices, with Fruquintinib showing improved OS when used earlier in the treatment sequence. These findings underscore the importance of exploring optimal sequencing strategies and evaluating Fruquintinib as a potential option before other approved agents in the refractory setting."

Clinical • HEOR • Metastases • Real-world • Real-world evidence • Colorectal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor • BRAF

Assessment of the Effects of Fruquintinib on Cardiac Safety in Patients with Metastatic Colorectal Cancer. (PubMed, J Clin Pharmacol) - P3 | "Additional C-QTc analysis, including only fruquintinib concentrations, showed no relationship between ΔQTcP and fruquintinib concentrations. The analysis indicated that fruquintinib administered at the approved clinical dose is not anticipated to cause clinically meaningful QT prolongation."

Journal • Colorectal Cancer • Oncology • Solid Tumor

Cardiovascular toxicity of fruquintinib in patients with colorectal and other cancers: A systematic review and meta-analysis. (ASCO 2025) - "Compared to Regorafenib, Fruquintinib demonstrated an OR of 1.549 (95% CI: 0.804, 2.983; P = 0.191) for the development of hypertension. Our study found that Fruquintinib is associated with significant cardiovascular risks, with hypertension being the most common adverse event, while thromboembolism did not reach statistical significance. Therefore, close monitoring for treatment-related cardiovascular events should be considered in these patients."

Retrospective data • Review • Cardiovascular • Colorectal Cancer • Congestive Heart Failure • Coronary Artery Disease • Heart Failure • Hypertension • Oncology • Peripheral Arterial Disease

Updated results of fruquintinib combined with PD-1 inhibitors and chemotherapy in the first-line treatment of HER2-negative advanced gastric or gastroesophageal junction adenocarcinoma (FDZL-FIX): A single-arm, open-label phase 2 study. (ASCO 2025) - P=N/A | "pts received 6 cycles of combined first line treatment with Fru (4mg p.o. qd, d1-14, q3w, ) combined with PD-1 inhibitor (investigator's choice of sintilimab 200mg or nivolumab 360mg intravenously q3w) and chemotherapy (investigator's choice of XELOX or SOX) regimen. The combination of fruquintinib and chemotherapy with PD-1 blockade in the first-line treatment for unresectable locally advanced or metastatic HER2-negative GC had shown promising efficacy and acceptable safety profile. The results warrant further investigations in a large cohort."

Clinical • Metastases • P2 data • Dermatology • Esophageal Cancer • Fatigue • Gastric Cancer • Gastroesophageal Junction Adenocarcinoma • Oncology • Solid Tumor • FLT1 • HER-2

Evaluating the efficacy of fruquintinib versus regorafenib and trifluridine/tipiracil in treating advanced metastatic colorectal cancer: A match-adjusted indirect comparison. (ASCO 2025) - P3 | "Our analyses showed favorable OS and PFS for fru versus reg and TAS102, as well as beneficial PFS in male versus reg, in K-Ras wild-type subgroup versus reg and TAS102, along with superior OS in < 65 years subgroup versus TAS102, highlighting its therapeutic potential in treating patients with previously treated mCRC. Limitations include the inability to adjust all covariances, biases due to unobserved covariances, and lacking comparison between reg and TAS102 due to unavailable IPDs. The findings should be validated through future RWS."

Clinical • Metastases • Colorectal Cancer • Oncology • Solid Tumor • KRAS • RAS

Fruquintinib in combination with camrelizumab and paclitaxel liposome and nedaplatin as first-line treatment for advanced esophageal squamous cell carcinoma (ESCC): A single-arm, phase II study. (ASCO 2025) - P1/2 | "The combination of fruquintinib, camrelizumab, paclitaxel liposome, and nedaplatin demonstrated significant efficacy and manageable toxicity profile as a first-line treatment for advanced ESCC, suggesting a potential new treatment strategy."

Clinical • Combination therapy • Metastases • P2 data • Anemia • Cardiovascular • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Hematological Disorders • Hypertension • Leukopenia • Mucositis • Neutropenia • Oncology • Pain • Squamous Cell Carcinoma • Stomatitis

Fruquintinib plus sintilimab and SOX as conversion therapy for initially unresectable gastric/gastroesophageal junction adenocarcinoma (GC/GEJC): Updated response and surgical results from a single-arm, phase 2 clinical trial. (ASCO 2025) - P2 | " Eligible pts were administered fruquintinib (4mg/d, po, qd, d1-14), sintilimab (200mg, iv, d1), oxaliplatin (130 mg/m2, iv, d1) and S-1 (40-60mg based on BSA, po, bid, d1-14) every 3 weeks for 3 or 6 cycles... Fruquintinib combined with sintilimab and SOX yielded quite high R0 conversion rate and R0 resection rate with a manageable safety profile in unresectable GC/GEJC, representing a potential and feasible conversion therapy regimen for this population. Survival data will continue to be followed up."

Clinical • P2 data • Anemia • Esophageal Cancer • Gastric Cancer • Gastroesophageal Cancer • Gastroesophageal Junction Adenocarcinoma • Hematological Disorders • Oncology • Pneumonia • Solid Tumor

Navigating third-line therapies: A comprehensive review of regorafenib versus fruquintinib with placebo comparator for metastatic colorectal cancer—A systematic review and meta-analysis. (ASCO 2025) - "Regorafenib and Fruquintinib offer similar clinical benefits in refractory mCRC, but Fruquintinib may have a more favorable toxicity profile, particularly for all-grade adverse events. These findings suggest that Fruquintinib could be a preferred option based on tolerability, though both agents remain essential therapeutic options in advanced mCRC."

Metastases • Retrospective data • Review • Colorectal Cancer • Oncology • Renal Disease • Solid Tumor

Analysis of serous carcinoma subgroup in FRUSICA-1: Fruquintinib plus sintilimab in treated advanced endometrial cancer (EMC) patients (pts) with pMMR status. (ASCO 2025) - P1/2 | "In these 27 pts, median age was 63.1 years, 22 (81.5%) pts were in stage Ⅳ disease, 7 (25.9%) pts had received prior bevacizumab therapy, and 5 (18.5%) pts had received prior pelvic radiotherapy. F+S was tolerable and showed clinically meaningful efficacy in endometrial serous carcinoma, characterized by durable responses that were comparable across the ITT population."

Clinical • Metastases • pMMR • Cardiovascular • Dermatology • Endometrial Cancer • Endometrial Serous Adenocarcinoma • Endometrial Serous Carcinoma • Hypertension • Oncology • Solid Tumor

Pharmacological Insights on USFDA-Approved Novel Drug Therapies in the Year 2023. (PubMed, Curr Drug Discov Technol) - "The novel drug therapies approved by the USFDA hold significant potential to enhance the patient's care by providing advanced treatment modalities. This manuscript, reporting the comprehensive description of therapeutic aspects of the mentioned new drug therapies, underscores the commitment of the pharmaceutical sector to address the unmet medical needs and reshape the landscape of the healthcare service system by instilling optimism among patients and healthcare providers."

FDA event • Journal • Pediatrics • Rare Diseases

First-Line Fruquintinib Combo May Offer New Treatment Strategy in ESCC (OncLive) - P1/2 | N=36 | NCT06010212 | "Frontline treatment with fruquintinib (Fruzaqla) plus camrelizumab, paclitaxel liposome, and nedaplatin elicited responses with an acceptable safety profile in patients with advanced esophageal squamous cell carcinoma (ESCC), according to findings from a phase 2 study (NCT06010212) presented during the 2025 ASCO Annual Meeting. Among evaluable patients (n = 19), the confirmed objective response rate (ORR) is 68.4% (95% CI, 47.5%-89.3%) by RECIST 1.1 criteria, which was comprised entirely of partial responses; 31.6% of patients had stable disease. The disease control rate (DCR) was 100.0% (95% CI, 82.4%-100.0%). Moreover, at a median follow-up of 5.1 months (95% CI, 4.2-7.2), the median progression-free survival (PFS) was 8.7 months (95% CI, 5.2-not reached); the 6-month PFS rate was 81.7%."

P2 data • Esophageal Squamous Cell Carcinoma