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fosaprepitant (Focinvez)

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SPES Pharmaceuticals · TACR1 · Small Molecule

What is fosaprepitant?

fosaprepitant is a small molecule developed by SPES Pharmaceuticals. It is approved for therapeutic indications via injectable (others) or intravenous (iv).

Drug Profile

Brand NamesFocinvez
CompanySPES Pharmaceuticals
Drug ClassSmall Molecule
Molecular TargetTACR1
RouteInjectable (Others), Intravenous (IV)
StatusApproved
Sources: ClinicalTrials.gov, SPES Pharmaceuticals

Mechanism of Action

Molecular Targets

fosaprepitant acts on 1 molecular target:

TACR1tachykinin receptor 1 (SPR, TAC1R)
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Related Research Articles

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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PubMedPDA journal of pharmaceutical science and technology2026-04-30

Root Cause Determination for Customer Complaint Biopharmaceutical Drug Product Samples with Abnormal Appearance.

Ma Yiwei Y, Liu Jian J, Gallegos Alejandra A, Lee Hans H et al.

Customer complaints due to drug product abnormalities may arise even with strict quality control measures at the manufacturing and healthcare provider levels, posing serious challenges for the manufacturers. In this paper, we report three compelling case studies which exemplify effectiveness of root cause analyses in addressing customer complaints of Amgen drug products. The three customer complaints from three different drug products reported the following issues: pink discoloration in one drug product vial, cloudy liquid with suspended particles in another drug product vial, and brown discoloration in the third drug product vial. Consequently, a comprehensive root cause analyses were performed to identify and rectify the underlying issue, thereby mitigating the recurrence of complaints. The root cause analysis of the three events ruled out manufacturing processes as the source of contamination. Instead, it was more likely that the contamination originated at the healthcare providers' facilities. Orthogonal analytical test methodologies were employed on the samples to identify any potential contaminants. The cloudy appearance, pink and brown discolorations in the three customers returned vials were caused by non-Amgen products. The first vial had cyanocobalamin injectable (vitamin B12), the second vial had fosaprepitant (a non-Amgen drug), and the third vial had iron and saline solution (likely injectable anemia drug). A possible explanation for the three complaint samples is that they were mishandled during the process of administering the drug products at the facilities of the healthcare providers. Following the identification of the likely sources of contamination, Amgen followed standard compliant-handling procedures, which may include communicating results back to complaints or health providers as appropriate. In conclusion, the pursuit of root cause determination is paramount in addressing customer complaints and ensuring the quality, safety, and efficacy of biopharmaceutical products.

PMID 42055945
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PubMedDrug design, development and therapy2026-03-16

Fosaprepitant versus Ondansetron for Preventing Postoperative Nausea and Vomiting After Video-Assisted Thoracoscopic Lung Resection: A Randomized Controlled Clinical Trial.

Qi Xiuqing X, Zhang Jinying J, Sun Jiaojiao J, Wang Xuyang X et al.

Postoperative nausea and vomiting (PONV) is a frequent complication after video-assisted thoracoscopic lung resection, particularly in patients at moderate to high risk, and substantially hinders recovery. Fosaprepitant, a neurokinin-1 (NK-1) receptor antagonist, is approved for PONV prevention; however, its efficacy in video-assisted thoracoscopic lung resection remains uncertain. This randomized trial evaluated the efficacy of fosaprepitant versus ondansetron in preventing PONV in high-risk patients undergoing video-assisted thoracoscopic lung resection. In this prospective, double-blind, randomized controlled clinical trial, 233 adults aged 18-70 years undergoing elective video-assisted thoracoscopic lung resection with an Apfel score ≥ 2 were randomized 1:1 to receive intravenous fosaprepitant 150 mg or ondansetron 8 mg, each combined with dexamethasone 5 mg. The primary outcome was the incidence of PONV at 24 hours postoperatively. Secondary outcomes included the incidence and severity of PONV at 6, 12, and 48 hours postoperatively, the use of rescue antiemetics, adverse events, and recovery outcomes. The 24-hour incidence of PONV was 31.0% [36] in the fosaprepitant group and 41.0% [48] in the ondansetron group (OR, 0.76; 95% CI, 0.53 to 1.07; P=0.112). Fosaprepitant significantly reduced PONV at 48 hours (10.3% [12] vs 20.5% [24]; OR, 0.51; 95% CI, 0.27 to 0.96; P=0.032), as well as vomiting at 24 hours (8.6% [10] vs 21.4% [25]; OR, 0.40; 95% CI, 0.20 to 0.80; P=0.006) and 48 hours (0% [0] vs 5.1% [6]; OR, 0.07; 95% CI, 0.00 to 1.32; P=0.040). Fosaprepitant was superior to ondansetron in preventing early postoperative vomiting and delayed-phase PONV, and it represents an effective antiemetic strategy for high-risk thoracic surgical patients. Registration number, NCT05881486; https://clinicaltrials.gov.

PMID 41836527
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PubMedPediatric blood & cancer2026-03-13

Intravenous Fosaprepitant Versus Oral Aprepitant for Children Receiving Highly Emetogenic Chemotherapy: An Investigator-Initiated Randomized, Open-Label, Non-Inferiority Trial.

Rasheed Azgar Abdul AA, Ganguly Shuvadeep S, Sra Manraj Singh MS, Kumar Santhosh S et al.

Fosaprepitant is non-inferior to aprepitant in adults receiving highly emetogenic chemotherapy (HEC). We evaluated whether fosaprepitant is non-inferior to aprepitant in children receiving HEC. In this open-label, non-inferiority trial, children aged 5-18 years, receiving their first cycle of HEC, were randomized 1:1 to the fosaprepitant or aprepitant group. The fosaprepitant group received a single intravenous dose of 4 mg/kg (max 150 mg). The aprepitant group received oral aprepitant capsules (weight 15 to <30 kg: 80 mg Days 1-3; weight ≥30 kg, or age ≥12 years: 125 mg Day 1, 80 mg Days 2 and 3). Both groups received ondansetron and dexamethasone. The primary outcome was the complete response (CR) rate of vomiting during the acute phase (AP) with a non-inferiority margin of 15%. Secondary outcomes included CR rates in the delayed (DP) and overall phases (OP), grade of vomiting, incidence and severity of nausea, and adverse effects. A total of 279 children were included in the modified intention-to-treat analysis (fosaprepitant group: 140; aprepitant group: 139). In AP, the difference of CR rate between fosaprepitant [76 (54.3%)] and aprepitant groups [84 (60.4%)] was -6.1% [90% CI: -15.7% to +3.6%], with the lower limit exceeding -15%, failing to establish non-inferiority. The CR rate with fosaprepitant versus aprepitant was 62.1% (n = 87) versus 65.5% (n = 91) in DP (difference: -3.4%; 90% CI: -12.7% to 6.1%) and 42.9% (n = 60) versus 49.6% (n = 69) in the OP (difference: -6.7%; 90% CI: -16.5% to 3.1%). Grade of vomiting, incidence and severity of nausea, and adverse effects were similar between the two groups. Non-inferiority of fosaprepitant compared to aprepitant was not demonstrated in children undergoing their first cycle of HEC. Clinical Trials Registry, India (CTRI/2019/05/019082).

PMID 41823195
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PubMedCurrent oncology (Toronto, Ont.)2026-02-26

Optimizing Antiemetic Strategies Across Phases of Chemotherapy-Induced Nausea and Vomiting: Real-World Evidence in Breast Cancer.

Doğan Akif A, Erölmez Hande Nur HN, Akdağ Goncagül G, Yıldırım Sedat S et al.

Chemotherapy-induced nausea and vomiting (CINV) remains one of the significant challenges in oncology despite guideline-based prophylaxis, particularly in patients receiving highly emetogenic chemotherapy (HEC). While neurokinin-1 (NK-1) receptor antagonists are established as a key component of standard antiemetic regimens, evidence of their phase-specific effectiveness in real-world, homogeneous patient populations remains limited. This study aimed to determine which antiemetic regimen provides optimal control in each CINV phase to support a tailored prophylactic approach. This single-center, retrospective, real-world study included 260 female patients with stage II-III breast cancer receiving anthracycline-cyclophosphamide-based HEC. All patients had similar demographic and clinical characteristics, forming a relatively homogeneous cohort. Each received a triple antiemetic regimen consisting of a 5-HT3 receptor antagonist, dexamethasone, and an NK-1 receptor antagonist (either a single-dose intravenous fosaprepitant or a 3-day oral aprepitant). Complete response (no vomiting and no rescue therapy) and no-vomiting rates were assessed in the acute (0-24 h), delayed (24-120 h), and overall (0-120 h) phases. In this relatively homogeneous cohort of high-risk patients, fosaprepitant-based prophylaxis achieved better symptom control during the acute phase, whereas aprepitant-based regimens were more effective in the delayed and overall phases. These findings suggest phase-specific variations in antiemetic effectiveness that reflect pharmacokinetic and administration-route differences rather than population heterogeneity. This real-world analysis demonstrates that antiemetic effectiveness varies by CINV phase, even within a relatively homogeneous, high-risk patient cohort. The results highlight the importance of phase-tailored prophylactic strategies to optimize symptom control and improve patient quality of life in highly emetogenic chemotherapy settings.

PMID 41744842
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PubMedBrain & development2026-02-21

Cyclic vomiting syndrome.

Hikita Toshiyuki T

Cyclic vomiting syndrome (CVS) is characterized by recurrent vomiting episodes. In this study, the mean ages at the onset of symptoms and at the diagnosis of children with cyclic vomiting pattern were 5.7 and 8.0 years, respectively. On average 2.3 years elapsed between the onset and diagnosis, suggesting the difficulty of diagnosing CVS. However, the prevalence of CVS ranges from approximately 0.3% to 2%. Its pathophysiology, prognosis, and natural history need to be further investigated. Various abortive and prophylactic therapies that have been applied in CVS cases were reported. To date, no randomized control study on abortive therapy (i.e., treatment intended to stop a migraine once it starts) for CVS has yet been conducted. Current treatment recommendations are detailed in the North American Society for Pediatric Gastroenterology, Hepatology, and Nutrition (NASPGHAN) 2025 guidelines for the management of CVS in children. The NASPGHAN 2025 guidelines for the management of CVS in children recommend non-steroidal anti-inflammatory drugs, triptans, ondansetron, aprepitant, and fosaprepitant for acute medicine. The NASPGHAN 2025 guidelines for the management of CVS in children recommend coenzyme Q10, riboflavin, and magnesium as preventive treatments. The recommended medications include propranolol, cyproheptadine, aprepitant, and amitriptyline. The guidelines also recommend not using the antiseizure medications topiramate and valproic acid. However, antiseizure medications are recommended only for patients who are unresponsive to the aforementioned preventive medications and who have frequent vomiting and severe symptoms.

PMID 41719916
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