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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

PubMedJournal of laparoendoscopic & advanced surgical techniques. Part A2026-10-23

Multimodal Antiemetic Prophylaxis in Patients Undergoing Endoscopic Sleeve Gastroplasty: A Single-Center Retrospective Case Series.

Izgi Murat M, Savran Ozgur Yildirim OY, Ozen Ozge O, Debbag Sehend S et al.

Endoscopic sleeve gastroplasty (ESG) is associated with a high incidence of postoperative nausea and vomiting (PONV) due to gastric volume reduction, preservation of vagal innervation, and inherent patient-related risk factors. Standard antiemetic prophylactic regimens are frequently insufficient in this population. This case series describes the clinical experience and postoperative outcomes associated with a multimodal antiemetic prophylaxis regimen. In this single-center retrospective case series, data from 20 adult patients who underwent ESG under general anesthesia were analyzed. Anesthesia maintenance was standardized using manually controlled intravenous infusions of propofol and remifentanil (TIVA), without volatile anesthetics. Multimodal antiemetic prophylaxis consisted of intravenous granisetron (3 mg), dexamethasone (8 mg), haloperidol (1 mg at induction + 1 mg before emergence), and fosaprepitant (150 mg). Postoperative analgesia was managed primarily with paracetamol and ibuprofen. The primary outcome was clinically documented PONV during the early postoperative period, including the PACU stay and the first 12 postoperative hours. Emergency department presentations for severe PONV within 5 postoperative days were assessed as a secondary outcome using institutional electronic health records. The cohort comprised 20 patients (70% female, mean age 41.05 ± 11.22 years, mean BMI 38.33 ± 4.94 kg/m2). Comorbidities were present in 55% of patients, and 80% were non-smokers. During the early postoperative period, no clinically documented episodes of PONV requiring rescue antiemetic treatment were identified. In this small retrospective case series, multimodal antiemetic prophylaxis combined with TIVA was associated with no institutionally documented early postoperative PONV presentations and emergency department presentations for severe PONV within 5 days after ESG. Prospective studies with standardized postoperative PONV assessment are needed to determine the efficacy of this approach. Given the limitations of a retrospective case series, prospective controlled trials incorporating systematic PONV severity scoring are warranted to establish optimized guidelines.

PMID 42914571
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PubMedSisli Etfal Hastanesi tip bulteni2026-10-02

Real-World Outcomes of Fosaprepitant-Containing Prophylaxis in Patients Receiving Highly and Moderately Emetogenic Chemotherapy: A Two-Center Retrospective Study.

Celayir Ozde Melisa OM, Korkmaz Taner T, Sonmez Ozlem O, Ataacar Aydınoglu Alara A et al.

This study aimed to evaluate the efficacy and safety of fosaprepitant-containing antiemetic prophylaxis and associated patient-related risk factors in patients receiving highly emetogenic chemotherapy (HEC) and moderately emetogenic chemotherapy (MEC). Medical records of patients treated between July 2021 and March 2022 at two oncology centers were retrospectively reviewed. A total of 50 adult patients receiving chemotherapy were included in the study. The antiemetic regimen consisted of fosaprepitant, dexamethasone, granisetron, and olanzapine. Demographic data, emetogenic risk classification, Beck Anxiety Inventory (BAI) scores, timing and frequency of nausea and vomiting according to NCI-CTCAE v5.0, the need for rescue antiemetics, and adverse events were evaluated. The primary endpoint was defined as complete response (no vomiting) within 0-120 hours. Statistical analyses were performed using Fisher's exact test. The majority of patients were female (80%) and younger than 65 years (84%). The most frequent diagnoses were breast cancer (38%) and pancreatic-biliary cancers (18%). All patients with comorbidities were in remission. A history of hyperemesis gravidarum was reported in 22% of patients, motion sickness in 18%, and alcohol use in 18%. Based on BAI scores, moderate and severe anxiety were detected in 16% and 2% of patients, respectively. According to the emetogenic risk classification, 82% of patients received HEC and 18% received MEC. Complete vomiting control was achieved in 80% of patients receiving fosaprepitant therapy, whereas 48% experienced no nausea. No statistically significant associations were found between emetogenic risk group, anxiety level, alcohol use, history of hyperemesis gravidarum, or motion sickness and treatment response (p>0.05). Complete response rates were 85.4% in the HEC group and 55.6% in the MEC group (p=0.118). Although the complete response rate was lower in patients with clinically significant anxiety (66.7%) than in those with low anxiety (82.4%), the difference was not statistically significant (p=0.475). Rescue antiemetics were required in 52% of patients. The most common adverse events were fatigue (10%) and dyspepsia (4%). In this real-world study, high rates of vomiting control were observed with fosaprepitant-based antiemetic therapy. The treatment was generally well tolerated. Although not statistically significant, the lower response rates observed in patients receiving MEC regimens and those with high anxiety levels suggest the need for more vigilant monitoring in these patient subgroups.

PMID 42824916
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PubMedScience translational medicine2026-09-23

Drug repurposing identifies candidate uterus-selective tocolytics for preterm labor.

Siricilla Shajila S, Hansen Christopher J CJ, Staub Jeremy J, Walker Jordan J et al.

At present, there are no US Food and Drug Administration (FDA)-approved tocolytics for the management of preterm labor. To identify drugs for repurposing as tocolytics, a phenotypic high-throughput screen against a library of 1191 FDA-approved drugs was performed for inhibitors of in vitro uterine myometrial contractions. A total of 51 drugs inhibited calcium (Ca2+) mobilization in primary human myometrial cells. To minimize potential off-target effects, hit drugs were counterscreened against primary human aortic vascular smooth muscle cells, identifying 10 uterine-selective drugs. Of these, two drugs, the antiemetic fosaprepitant dimeglumine and the glucocorticoid ciclesonide, displayed favorable in vitro therapeutic indices (TIs > 5), inhibited contractions in human myometrial tissue ex vivo, and did not alter tone in the fetal murine ductus arteriosus ex vivo. Next, the potential synergy among hit drugs and clinically used tocolytics was evaluated using a high-throughput combination screen based on Ca2+ mobilization in primary human myometrial cells. Four synergistic drug combinations incorporating ciclesonide, indomethacin, ivermectin, atosiban, or nelfinavir mesylate displayed favorable TIs of >5 and improved ex vivo tocolytic potency, efficacy, or both. Last, aprepitant, ciclesonide, and four synergistic drug combinations delayed delivery until term and improved neonatal viability and skin and lung maturation in a mouse model of induced preterm labor, with several combinations outperforming their component drugs. This approach established a systematic strategy for identifying uterus-selective tocolytics, and these findings support further preclinical development of repurposed drugs and drug combinations for the treatment of preterm labor to improve pregnancy and neonatal outcomes.

PMID 42777085
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PubMedSurgical endoscopy2026-09-18

Comparison of aprepitant 80 mg oral, aprepitant 32.4 mg intravenous, and fosaprepitant 75 mg intravenous in the prevention of postoperative nausea and vomiting in patients undergoing laparoscopic sleeve gastrectomy, a retrospective cohort study.

Dahman Mohamed M, Ratermann Craig C, Stuart Faith F, King Kylie K

The most common postoperative (post-op) complication in bariatric surgery is postoperative nausea and vomiting (PONV) with up to 70% of patients reporting symptoms. PONV is also associated with longer post-anesthesia care unit (PACU) time and hospital stays overall. Aprepitant has shown efficacy in reducing PONV and has been added to many standard antiemetic regimens; however, the bioavailability of the oral formulation is not ideal in bariatric surgery patients, and the ideal dose intravenously (IV) has not been established. This retrospective cohort study compared aprepitant 80 mg orally (PO) to aprepitant 32.4 mg intravenous (IV) and fosaprepitant 75 mg IV. The presence of PONV was defined by the number of doses of antiemetics administered postoperatively within four windows: PACU plus 1 h, defined as time upon entry to PACU+1 h, PACU + 12 h, PACU + 24 h, and any further doses administered while admitted thereafter. Secondary outcomes included time to diet ordered, length of hospital stay, and pain control. There was no difference in PONV between aprepitant 80 mg PO vs. 32.4 mg IV vs. fosaprepitant 75 mg in the immediate interim after surgery (PACU + 1 h); however, fosaprepitant was statistically superior to the other two groups at PACU + 12 h, PACU + 24 h, and total doses administered throughout admission. There was no difference in time to diet ordered or pain control, but fosaprepitant was superior when looking at length of stay. In this retrospective cohort, fosaprepitant 75 mg IV was found to be superior overall to aprepitant 32.4 mg IV and 80 mg PO.

PMID 42754628
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PubMedBMJ supportive & palliative care2026-08-28

Cost-effectiveness analysis of fosaprepitant versus aprepitant-based antiemetic regimens in children receiving highly emetogenic chemotherapy: individual patient-level analysis of a randomised trial.

Kumar Rahul R, Sra Manraj Singh MS, Rasheed Azgar Abdul AA, Sasi Archana A et al.

To assess the trial-based cost-effectiveness of an intravenous fosaprepitant-based antiemetic regimen compared with oral aprepitant, in combination with ondansetron and dexamethasone, among children receiving highly emetogenic chemotherapy in India and the USA using individual patient-level data. Costs were estimated from a private payer perspective in India and the USA. Health outcomes were expressed as quality-adjusted life-years (QALYs). Incremental cost-utility ratio (ICUR) and incremental net monetary benefit (iNMB) were calculated. Uncertainty was evaluated through one-way deterministic sensitivity analyses. A total of 140 and 139 children were enrolled in the fosaprepitant and aprepitant groups, respectively. Mean QALYs were marginally higher in the aprepitant group (0.0118 vs 0.0116; difference: 0.0002). In India, mean costs were $33.94 in the fosaprepitant arm vs $19.73 in the aprepitant arm (difference: $14.21). In the USA, mean costs were $615.92 vs $809.73, respectively, in the two arms (difference: $193.81), favouring fosaprepitant. iNMB values of fosaprepitant compared with aprepitant were -$15.59 in India and $173.81 in the USA, indicating lack of cost-effectiveness for fosaprepitant in India but cost-effectiveness in the USA. In sensitivity analyses, the ICUR was most sensitive to the cost of fosaprepitant in India and to the utility value of the complete protection health state in the USA. Intravenous fosaprepitant, administered in combination with ondansetron and dexamethasone, was not cost-effective compared with oral aprepitant-based combination therapy in India but demonstrated cost-effectiveness in the USA.

PMID 42660630
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PubMedJournal of clinical oncology : official journal of the American Society of Clinical Oncology2026-07-31

Dexamethasone-Free Antiemetic Prophylaxis for Children and Adolescents Receiving Highly Emetogenic Chemotherapy: A Multicenter, Phase III, Noninferiority Trial (CIVIC POD).

Radhakrishnan Venkatraman V, Srinivasan Prasanth P, Das Gargi G, Bakhshi Sameer S et al.

Dexamethasone combined with a 5-hydroxytryptamine-3 receptor antagonist and a neurokinin-1 receptor antagonist is the guideline-recommended prophylaxis for chemotherapy-induced nausea and vomiting (CINV) in children receiving highly emetogenic chemotherapy (HEC), but it is associated with clinically relevant toxicities. The role of olanzapine as a dexamethasone-sparing agent for pediatric CINV prophylaxis remains uncertain. The Chemotherapy Induced Vomiting in Children-Prophylaxis Omitting Dexamethasone (CIVIC POD) was an investigator-initiated, multicenter, open-label, phase III, randomized noninferiority (NI) trial (INPHOG-SUPP-22-03) that enrolled patients age 4-18 years scheduled to receive single- or multiday HEC. Patients were randomly assigned 1:1 to dexamethasone, palonosetron, and fosaprepitant (DEX) or olanzapine, palonosetron, and fosaprepitant (OLANZ) for one chemotherapy cycle. The primary end point was complete response (CR) to vomiting (no vomiting and no rescue antiemetics) during the overall period (0-120 h after last chemotherapy). The prespecified NI margin was -15%. A total of 310 patients were randomly assigned (DEX, n = 156; OLANZ, n = 154). The median age was 13 years, 62.3% were male, and 51.9% received multiday chemotherapy. The per-protocol population included 299 patients (DEX, n = 151; OLANZ, n = 148). The overall-period CR to vomiting was 56.9% with DEX and 63.5% with OLANZ (absolute difference, 6.6% [95% CI, -4.5 to 17.7]), meeting NI criteria. Acute-period CR to vomiting was 64.2% versus 68.9%, and delayed-period CR was 78.8% versus 79.1% (DEX v OLANZ). CR to nausea during the overall, acute, and delayed periods was 54.3% versus 53.4%, 59.6% versus 59.5%, and 69.5% versus 68.9%, respectively. Any-grade somnolence was more frequent with OLANZ (50.7% v 17.2%). A dexamethasone-free regimen using olanzapine demonstrated noninferior control of vomiting compared with standard prophylaxis in children and adolescents receiving HEC, supporting olanzapine as a potential corticosteroid-sparing alternative for pediatric CINV prophylaxis.

PMID 42535876
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