Benefits and Risks of Fosaprepitant in Patients Receiving Emetogenic Regimens

Pritchett, Wendy; Kinsley, Karen

doi:10.1188/16.cjon.555-556

Cited by 7 publications

(11 citation statements)

References 6 publications

(8 reference statements)

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“…3). In contrast, such inflammation at the vascular tissue was not observed in the FAP-D and AP groups in the present study, even though it was reported that FAP alone and EPI alone can cause infusion site adverse events (4–9). In clinical practice, complaints of vascular pain from patients also appeared after switching from oral AP to intravenous FAP.…”

Section: Discussioncontrasting

confidence: 86%

“…AP is taken orally and FAP is administered intravenously to prevent systemic adverse events such as nausea and vomiting. Oral AP is ingested once before and twice after EPI treatment, once/day for 3 days mostly for inpatients, and intravenous FAP is administered once by constant-rate infusion over 30 min just before EPI treatment mostly for outpatients (4). It has been reported that intravenous FAP alone and an intravenous anthracycline such as doxorubicin alone can cause infusion-site adverse events (4–9).…”

Section: Introductionmentioning

confidence: 99%

“…Oral AP is ingested once before and twice after EPI treatment, once/day for 3 days mostly for inpatients, and intravenous FAP is administered once by constant-rate infusion over 30 min just before EPI treatment mostly for outpatients (4). It has been reported that intravenous FAP alone and an intravenous anthracycline such as doxorubicin alone can cause infusion-site adverse events (4–9). In addition, the combined use of FAP and an anthracycline is reported to induce infusion-site adverse events such as vascular pain and venous inflammation with high probability (10–12).…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Study on the infusion‑site adverse events and vascular distribution of epirubicin in chemotherapy with epirubicin and fosaprepitant

et al. 2019

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In breast cancer patients on a fluorouracil-epirubicin (EPI)-cyclophosphamide (FEC) regimen and intravenous fosaprepitant (FAP) during chemotherapy, infusion-site adverse events such as vascular pain and induration and/or phlebitis are observed. In the present study, adverse events induced by the FEC regimen and FAP, a prodrug of aprepitant (AP), were studied based on the vascular tissue distribution of EPI in rats. Rats were treated with intravenous FAP (3 mg/kg, 10 min-constant rate infusion) or oral AP (3 mg/kg) and then intravenous EPI (1 mg/kg, 5 min-constant rate infusion) as follows: FAP-S Group, FAP and then EPI was infused from the same site on the jugular vein; FAP-D Group, FAP and then EPI was infused from different jugular veins (left and right); and AP Group, AP was administered orally and EPI was infused from the jugular vein. Concentrations of EPI in vascular tissue at the EPI infusion sites and opposite sites of the jugular vein (left and right, respectively) were measured at 30 min and 24 h after EPI infusion. Histological observation of the EPI infusion site was also made separately. In rats, the tissue concentrations of EPI at the infusion site in the FAP-S group were higher than those in the FAP-D and AP groups. Inflammation and necrosis were observed at the EPI infusion-site vascular tissue of the FAP-S group, but not of the FAP-D and AP groups. These findings could aid the development of an approach to avoid infusion-site adverse events in anthracycline-based chemotherapy in the clinical practice.

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Section: Discussioncontrasting

confidence: 86%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Study on the infusion‑site adverse events and vascular distribution of epirubicin in chemotherapy with epirubicin and fosaprepitant

et al. 2019

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“…Fosaprepitant is a neurokinin 1 receptor (NK-1R) antagonist that binds and deactivate NK-1R leading to downstream effect such as Ca 2+ signaling through the g-protein coupled receptor (GPCR) cascade, which in turn leads to cellular sequestration resulting in vomiting [24][25][26] . Fosaprepitant exerts its effect on targeted cells by passing across the blood brain barrier (BBB) to its target destination 23 .…”

Section: Discussionmentioning

confidence: 99%

Structural insights of human N-acetyltransferase 10 and identification of its potential novel inhibitors

Dalhat

Altayb

Khan

et al. 2021

Sci Rep

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N-acetyltransferase 10 (NAT10), is an acetyltransferase that regulates RNA stability and translation processes. Association of NAT10 with several diseases including cancer, makes it a promising therapeutic target. Remodelin is the only known NAT10 inhibitor, but the structural information related to its binding with NAT10 is still obscure. Here, we predicted the human NAT10 structure using homology modeling that was not available previously and used human NAT10 to identify the novel binding site(s) of Remodelin. The alignment of the modeled human NAT10 showed 24% identity and 37% positivity with crystal structure of tRNA (Met) cytidine acetyltransferase. Molecular docking showed binding of Remodelin with NAT10 in acetyl-CoA binding pocket. Additionally, we screened a library of FDA-approved drugs for the identification of novel inhibitors of NAT10 activity. Binding score showed that four drugs namely, Fosaprepitant (− 11.709), Leucal (− 10.46), Fludarabine (− 10.347) and Dantrolene (− 9.875) bind to NAT10 and have better binding capability when compared with Acetyl-CoA (− 5.691) and Remodelin (− 5.3). Acetyl-CoA, Remodelin, and others exhibit hits for hydrophobic, hydrophilic and hydrogen interactions. Interestingly, Remodelin and others interact with the amino acid residues ILE629, GLY639, GLY641, LEU719, and PHE722 in the Acetyl-CoA binding pocket of NAT10 similar to Acetyl-CoA. Our findings revealed that Fosaprepitant, Leucal, Fludarabine, and Dantrolene are promising molecules that can be tested and developed as potential inhibitors of NAT10 acetyltransferase activity.

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“…5 Docetaxel has also demonstrated efficacy and tolerability in the neoadjuvant treatment of operable breast cancer. 6,7 The conventional formulation of docetaxel has several toxicity issues related to its excipients, polysorbate 80 and ethanol, such as acute hypersensitivity reactions, 8,9 cumulative fluid retention, 10 peripheral neuropathy, 11 severe anaphylactoid reactions, 12 infusion-site reactions, 13 and alcohol intoxication. 14,15 Corticosteroids and antihistamines are used as premedication to overcome these toxicities, [16][17][18] but these adverse effects may still occur in some patients.…”

Section: Introductionmentioning

confidence: 99%

<p>Nanosomal Docetaxel Lipid Suspension-Based Chemotherapy in Breast Cancer: Results from a Multicenter Retrospective Study</p>

Subramanian

Prasanna²,

Biswas

et al. 2020

BCTT

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The purpose of this study was to evaluate the efficacy and safety of nanosomal docetaxel lipid suspension (NDLS, DoceAqualip)-based chemotherapy in breast cancer. Methods: Medical charts of patients with breast cancer, who were treated and followed up with NDLS (75-100 mg/m 2 ; 3-week cycle)-based chemotherapy from August 2014 to September 2018, were analyzed in this multicenter, retrospective study. The study endpoints were overall response rate (ORR: complete response [CR]+partial response [PR]) and disease control rate (DCR: CR+PR+stable disease [SD]) in neoadjuvant and metastatic settings. Overall survival (OS) and safety were evaluated for all settings. Results: Of 91 patients (neoadjuvant: 12, adjuvant: 61, metastatic: 18), efficacy evaluation in 29 patients (neoadjuvant: 12/12, metastatic: 17/18) demonstrated an ORR and DCR of 100%, respectively, in the neoadjuvant setting, and an ORR of 64.7% and DCR of 70.6%, respectively, in the metastatic setting. At a median follow-up of 21.6 months (range: 2.1 to 49.9 months), median OS was not reached in neoadjuvant and adjuvant settings, and it was 30.4 months in metastatic settings. At least one adverse event (AE) was reported in 59.3% of patients. Anemia, thrombocytopenia, lymphopenia, and neutropenia were the most common hematological AEs reported while hyperglycemia and alteration in liver function tests were the most common non-hematological AEs. NDLS-based treatment was well tolerated without any new safety concerns. Conclusion: Nanosomal docetaxel lipid suspension-based chemotherapy was efficacious and well tolerated in the treatment of breast cancer. Further, NDLS is being evaluated prospectively in patients with triple-negative breast cancer (ClinicalTrials.gov: NCT03671044).

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Benefits and Risks of Fosaprepitant in Patients Receiving Emetogenic Regimens

Cited by 7 publications

References 6 publications

Study on the infusion‑site adverse events and vascular distribution of epirubicin in chemotherapy with epirubicin and fosaprepitant

Study on the infusion‑site adverse events and vascular distribution of epirubicin in chemotherapy with epirubicin and fosaprepitant

Structural insights of human N-acetyltransferase 10 and identification of its potential novel inhibitors

<p>Nanosomal Docetaxel Lipid Suspension-Based Chemotherapy in Breast Cancer: Results from a Multicenter Retrospective Study</p>

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