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fosaprepitant (Focinvez)

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SPES Pharmaceuticals · TACR1 · 小分子

什么是 fosaprepitant？

fosaprepitant 是一种小分子，由SPES Pharmaceuticals研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intravenous (IV)。

药物档案

商品名Focinvez
公司SPES Pharmaceuticals
药物类别小分子
分子靶点TACR1
给药途径Injectable (Others), Intravenous (IV)
状态Approved
来源： ClinicalTrials.gov, SPES Pharmaceuticals

作用机制

分子靶点

fosaprepitant 作用于 1 个分子靶点：

TACR1tachykinin receptor 1 (SPR, TAC1R)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

相关研究文献

PubMedCurrent oncology (Toronto, Ont.)2026-07-27

Aprepitant and Fosaprepitant for Preventing Nausea and Vomiting in Patients Receiving Highly Emetogenic Chemotherapy-A Real-World Study.

Ünlü Beyza B, Demir Hacer H, Davarcı Sena Ece SE, Culha Yaşar Y et al.

Chemotherapy-induced nausea and vomiting substantially impair patients' quality of life despite considerable advances in supportive care. Neurokinin-1 receptor antagonists, including oral aprepitant and intravenous fosaprepitant, constitute essential components of antiemetic regimens for highly emetogenic chemotherapy. In this prospective, non-randomized observational study, we compared the efficacy of oral aprepitant and intravenous fosaprepitant administered in combination with 5-hydroxytryptamine-3 receptor antagonists and dexamethasone in 136 chemotherapy-naive patients receiving cisplatin- or doxorubicin-cyclophosphamide-based regimens. Complete response rates during the acute (0-24 h), delayed (24-120 h), and overall (0-120 h) phases were comparable between the two groups, with no statistically significant differences in emesis severity. Multivariable analyses further demonstrated similar effectiveness irrespective of age, sex, or chemotherapy regimen. These findings indicate that no statistically significant differences in antiemetic efficacy were observed between aprepitant and fosaprepitant in routine clinical practice. Fosaprepitant may therefore represent a practical alternative when oral administration is not feasible.

PMID 42505183
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PubMedCancer management and research2026-06-11

Comparative Efficacy of Fosnetupitant and Fosaprepitant for Delayed Vomiting in Patients Receiving Irinotecan-Oxaliplatin Combination Chemotherapy: A Retrospective Propensity Score-Matched Study.

Maeda Kazuki K, Kawada Kei K, Hayashi Toshinobu T, Koyama Sota S et al.

Appropriate prevention of chemotherapy-induced nausea and vomiting (CINV) is essential for improving patients' quality of life; however, no studies have compared neurokinin-1 receptor antagonists in regimens combining oxaliplatin and irinotecan. We aimed to compare the antiemetic efficacy of fosnetupitant and fosaprepitant in patients receiving FOLFIRINOX or FOLFOXIRI regimens. We reviewed records of patients receiving FOLFIRINOX or FOLFOXIRI between April 1, 2018 and September 30, 2024 at Tokushima University Hospital. Eligible patients completed the first chemotherapy cycle, received standard triple antiemetic prophylaxis, and had complete nursing-recorded CINV follow-up data for days 1-7. Patients were matched 1:1 using propensity scores for age, sex, alcohol consumption history, prior treatment, regimen, and chemotherapy doses. The primary objective was to compare the incidence of vomiting during the long-delayed phase (days 6-7) between the fosnetupitant and fosaprepitant groups. The no-vomiting and no-nausea rates were compared using Fisher's exact test, and the time to first vomiting using the Log rank test. After matching, data from 68 balanced patient pairs were analyzed. The fosnetupitant group had higher no-vomiting rates in the long-delayed phase (100% vs. 91.2%, p=0.028) and overall period (95.6% vs. 83.8%, p=0.045), compared with the fosaprepitant group. No significant intergroup difference was observed in the overall no-nausea rate (26.5% vs. 32.3%, p=0.573). With fosnetupitant, the time to first vomiting was longer (3/68 vs. 11/68, hazard ratio: 0.20, p=0.045), injection site reactions were fewer (0.0% vs. 19.1%, p<0.001), and constipation and hiccup incidences were fewer (p>0.05). Despite the retrospective design, possible calendar-time confounding, and limited number of events, our results suggest that fosnetupitant offers better control of long-delayed and overall vomiting and a favorable safety profile, compared with fosaprepitant, in patients receiving FOLFIRINOX/FOLFOXIRI regimens.

PMID 42273006
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PubMedEuropean journal of clinical pharmacology2026-06-10

Efficacy of NEPA for prevention of chemotherapy induced nausea and vomiting in head and neck cancer patients receiving cisplatin-based chemotherapy.

Hwang Tzer-Zen TZ, Wang Chih-Chun CC, Yang Chuan-Chien CC, Lien Ching-Feng CF et al.

A 5-hydroxytryptamine-3 receptor antagonist (5-HT3RA) in combination with a neurokinin-1 receptor antagonist (NK-1RA) are effective for the prevention of chemotherapy induced nausea and vomiting. We investigated the efficacy between oral netupitant and palonosetron (NEPA) and intravenous fosaprepitant and palonosetron (FOPA) in recurrent or metastatic head and neck squamous cell carcinoma (R/M HNSCC) patients treated with cisplatin-based chemotherapy. R/M HNSCC patients who were treated with cisplatin-based chemotherapy as first-line treatment were enrolled in our study. All patients were stratified according to anti-emetic agents, classifying into NEPA group and FOPA group. Anti-emetic efficacy, patients self-report scores and hospitalization days were compared between NEPA and FOPA. A total of 425 R/M HNSCC patients were recruited into our study, with 211 patients in NEPA and 214 patients in FOPA. Anti-emetic efficacy were all significantly better with NEPA than with FOPA across cycle 1 to 5. The mean nausea score were 2.9 vs. 3.4 (p = 0.004) and the mean vomiting score were 1.4 vs. 2.7 (P = 0.001) in cycle 1 for NEPA group and FOPA group, respectively. The mean satisfaction scores were 8.5 vs. 8.2 ( P = 0.032) in cycle1 for NEPA group and FOPA group, respectively. Furthermore, the mean hospitalization days were shorter in NEPA than those in FOPA across cycle 1 to 5, with mean hospitalization days 6.0 versus 7.0 days in cycle 1, respectively. Oral NEPA exhibited a superior anti-emetic efficacy than intravenous FOPA, as well as shorter hospitalization days for R/M HNSCC patients treated with cisplatin-based chemotherapy.

PMID 42268415
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PubMedAnticancer research2026-05-28

Fosnetupitant Versus Fosaprepitant for Delayed Vomiting Upon Irinotecan-Oxaliplatin Combination Chemotherapy for Pancreatic/Colorectal Cancer.

Maeda Kazuki K, Koyama Sota S, Kawada Kei K, Hayashi Toshinobu T et al.

Real-world comparative data on neurokinin-1 receptor antagonists are needed among patients receiving FOLFOXIRI or FOLFIRINOX. We aimed to evaluate the antiemetic effectiveness of fosnetupitant versus that of fosaprepitant in patients treated with FOLFOXIRI/FOLFIRINOX regimens for pancreatic/colorectal cancer. This single-center retrospective study included patients treated from April 2018 to September 2024. Patients were matched 1:1 between treatment groups via propensity scores based on age, sex, alcohol history, prior treatment, and regimen dose, as appropriate. Antiemetic effectiveness was assessed as no vomiting/no nausea during days 1-7; safety outcomes were also evaluated. Inverse probability of treatment weighting (IPTW) was conducted to validate the robustness of the results. Between-group comparisons were performed using Fisher's exact tests for categorical variables and Mann-Whitney U-tests for continuous variables. After matching, 43 patient pairs in the pancreatic cancer cohort and 28 pairs in the colorectal cancer cohort were analyzed; the groups had generally comparable baseline characteristics. In the pancreatic cancer cohort, fosnetupitant was associated with higher no-vomiting rates during the long-delayed phase (100% vs. 81%, p=0.006) and overall period (95% vs. 74%, p=0.014) than fosaprepitant. No significant differences in effectiveness were observed in the colorectal cancer cohort. Injection site reactions were significantly less frequent with fosnetupitant in the colorectal cancer cohort (4% vs. 29%, p=0.025). These findings remained consistent in the IPTW sensitivity analysis. The effectiveness of fosnetupitant may vary according to cancer type, suggesting the need to tailor antiemetic strategies for patients receiving irinotecan-oxaliplatin combination chemotherapy.

PMID 42203343
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PubMedCancers2026-05-27

Efficacy and Safety of Oral NEPA Versus Fosaprepitant Plus Palonosetron for Preventing Chemotherapy-Induced Nausea and Vomiting in Patients with Nasopharyngeal Carcinoma: A Propensity-Score-Matched Retrospective Study.

Cai Yilin Y, Zeng Ying Y, Li Qihang Q, Yi Guihua G et al.

Objectives: This study compared the efficacy and safety of a single oral dose of a fixed-dose combination of netupitant and palonosetron (NEPA) with an intravenous regimen of fosaprepitant (FosAPR, 150 mg) plus palonosetron (PALO, 0.25 mg) in patients with locally advanced nasopharyngeal carcinoma (LA-NPC). Methods: This single-center retrospective cohort study included patients with stage III-IVa NPC who received cisplatin-based induction chemotherapy (IC) followed by concurrent chemoradiotherapy (CCRT) from January 2020 to October 2025. Propensity score matching (PSM) generated 214 patients per group. All patients also received olanzapine and dexamethasone. Complete response (CR, defined as no emesis and no rescue medication), nausea control, adverse events, and nutritional status changes were assessed across the acute, delayed, overall, and extended (0-168 h) phases. Results: After PSM, 214 patients were included in each group. During the first IC cycle, the oral NEPA group achieved a higher CR rate in the extended overall phase (0-168 h) than the FosAPR + PALO group (80.0% vs. 70.1%, p = 0.019). A similar difference was seen in the first CCRT cycle (74.8% vs. 64.5%, p = 0.021). The advantage persisted across subsequent cycles, with no between-group difference in the acute phase. Nausea control also favored oral NEPA: rates of no significant nausea (visual analog scale < 25 mm) during the extended overall phase were 77.1% versus 65.9% in the first IC cycle (p= 0.010) and 72.9% versus 60.3% in the first CCRT cycle (p = 0.006). Fewer patients in the NEPA group required rescue antiemetics (14.5% vs. 22.0% in the first IC cycle, p = 0.045), and the median time to first rescue was longer (58.3 vs. 51.3 h, p < 0.001). Adverse event profiles were similar between groups, with constipation being the most common. Nutritional outcomes, including weight loss ≥ 5% and severe malnutrition, did not differ significantly. Conclusions: For patients with LA-NPC receiving highly emetogenic chemotherapy (HEC), oral NEPA appears to offer superior and sustained chemotherapy-induced nausea and vomiting (CINV) prophylaxi with a simplified administration schedule compared with the intravenous FosAPR plus PALO regimen. These findings warrant confirmation in prospective studies.

PMID 42192892
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PubMedInternational journal of biological macromolecules2026-05-22

Inhibition of the oncogenic GTPase dynamin-related protein 1 (DRP1) by the FDA-approved drug fosaprepitant: In silico, biophysical, and in vitro characterization of its anti-myeloma activity.

Marchese Emanuela E, Murfone Pierpaolo P, Valentino Ilenia I, Cantafio Maria Eugenia Gallo MEG et al.

Mitochondrial fission plays a crucial role in sustaining cellular homeostasis, and disturbances in this process have been linked to numerous pathological conditions, including cancer. The central regulator of mitochondrial division is the large GTPase dynamin-related protein 1 (DRP1), whose enzymatic activity drives the constriction and separation of mitochondria. Given its pivotal function, DRP1 has gained attention as a potential oncogenic target across several cancer types. However, the availability of small-molecule inhibitors targeting DRP1 remains limited. To discover novel inhibitors, we performed a virtual screening campaign of FDA-approved drugs obtained from the DrugBank database, leading to the identification of three compounds predicted to interact with the GTPase domain of DRP1. Among these, the antiemetic agent fosaprepitant emerged as a promising hit. Computational docking and GTPase activity assays supported its inhibitory potential, which was further confirmed through saturation transfer difference nuclear magnetic resonance (STD-NMR) spectroscopy, demonstrating direct binding between fosaprepitant and DRP1 and elucidating key contact sites. Consistent with inhibition of mitochondrial fission, fosaprepitant treatment in multiple myeloma (MM) cell lines induced mitochondrial hyperfusion, decreased cell viability and colony formation in a DRP1-dependent manner, and disrupted oxidative phosphorylation (OXPHOS), ultimately leading to mitochondrial dysfunction and apoptotic cell death. Overall, this study provides a robust platform for the identification of novel DRP1 inhibitors among FDA-approved compounds, highlighting fosaprepitant as a promising candidate for drug repurposing with anti-cancer potential.

PMID 42167430
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