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aviptadil + phentolamine mesylate (Invicorp / VIP, Senetek / Resurgam)

✓ Approved

Johnson & Johnson Services, Inc. · VIPR1 · 小分子

什么是 aviptadil + phentolamine mesylate？

aviptadil + phentolamine mesylate 是一种小分子，由Johnson & Johnson Services, Inc.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Invicorp, VIP, Senetek, Resurgam
公司Johnson & Johnson Services, Inc.
药物类别小分子
分子靶点VIPR1
给药途径Injectable (Others), Intravenous (IV)
状态Approved
来源： ClinicalTrials.gov, Johnson & Johnson Services, Inc.

作用机制

分子靶点

aviptadil + phentolamine mesylate 作用于 1 个分子靶点：

VIPR1vasoactive intestinal peptide receptor 1 (PACAP-R2, V1RG)
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。

治疗适应症

aviptadil + phentolamine mesylate 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Reproductive system and breast disordersErectile dysfunction✓ Approved

相关研究文献

PubMedFrontiers in medicine2026-07-30

Case Report: Navigating the bleeding-thrombosis paradox: regional nafamostat anticoagulation in a post-intracerebral hemorrhage patient on VV-ECMO.

Zhang Shujia S, Zhang Zhenyin Z, Yang Jin J, Peng Jiangqiong J et al.

Extracorporeal membrane oxygenation (ECMO) in patients following intracerebral hemorrhage (ICH) poses a critical dilemma between circuit thrombosis and catastrophic rebleeding. While nafamostat mesylate (NM) has been increasingly explored for ECMO anticoagulation in patients with ICH, it is conventionally administered as a systemic anticoagulant with high activated partial thromboplastin time (aPTT) targets, which still carries significant bleeding risks. Moreover, whether NM can achieve effective regional anticoagulation in venovenous (VV) ECMO remains highly controversial. Here, we present a post-ICH patient with severe ARDS who required VV-ECMO. Due to suspected rebleeding, anticoagulation was transitioned from heparin to an anticoagulant-free strategy, which subsequently led to significant oxygenator thrombosis. To navigate this crisis, NM was initiated with an ultra-low systemic target, but it initially failed to establish a regional anticoagulant effect when infused at the conventional pre-membrane, post-pump site. Crucially, relocating the NM infusion to the pre-pump position successfully established a significant circuit-to-systemic aPTT gradient. This technical optimization enabled effective circuit anticoagulation while minimizing systemic bleeding risk, allowing for successful ECMO weaning without bleeding complications. This dynamic intra-patient observation highlights the potential impact of infusion site on coagulation outcomes. We hypothesize that harnessing the centrifugal pump's high-shear turbulence for homogenous drug mixing might serve as a crucial prerequisite for achieving regional anticoagulation in VV-ECMO. These findings bridge the gap between theoretical pharmacology and practical circuit engineering, offering a practical preliminary reference for the future anticoagulant management of similar high-bleeding-risk patients on ECMO.

PMID 42529180
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PubMedACS omega2026-07-28

Repurposing Masitinib Mesylate as a Novel FOXM1 Inhibitor for the Treatment of Aggressive Solid Tumors: Preclinical Validation in Human Breast and Oral Cancer Cells and Organotypic Tumor Slice Culture.

Gupta Rajat R, Singh Jai J, Shetty Shruti Dayanand SD, Kumar Naveena A N NAN et al.

The Forkhead box M1 (FOXM1) transcription factor, recognized as a prominent oncogene, facilitates cell cycle progression and mitotic fidelity in aggressive cancers. Overexpression of FOXM1 is correlated with uncontrolled cell proliferation, metastasis, and poor prognosis. Despite its pivotal role in promoting genomic instability, cancer stemness, and metastasis, FOXM1 remains a clinically undruggable target. In this study, we identified masitinib mesylate, a small-molecule inhibitor known for its multitargeted tyrosine kinase inhibition, targeting c-Kit, PDGFRα, and PDGFRβ, as well as Lyn, which demonstrates anticancer activity in preclinical models. Masitinib mesylate emerges as a potent, novel first-in-class small-molecule inhibitor of FOXM1. In silico prediction using pharmacophore-based virtual screening revealed that masitinib mesylate binds with high affinity to the FOXM1 DNA-binding domain (DBD) through hydrogen bonding with residues at His287 and Leu291, as well as a salt bridge with Asp293, effectively stabilizing the FOXM1-DNA interface and perturbing its activity. In vitro validation in the triple-negative breast cancer cell line MDA-MB-231 and the highly aggressive oral cancer cell line HSC-3 demonstrated that masitinib mesylate significantly reduces FOXM1 protein expression, thereby contributing to reduced cancer cell proliferation, stemness, and migration. Importantly, we validated these findings using ex vivo human primary tumor slice cultures from patients with breast cancer and oral squamous cell cancer. Treatment with masitinib mesylate significantly induced apoptosis within the native tumor microenvironment, confirming its efficacy in heterogeneous, patient-derived tissues. Our findings establish a novel mechanistic link between masitinib mesylate and FOXM1 inhibition by DNA binding, providing a compelling rationale for drug repurposing, offering a targeted therapeutic strategy to disrupt the FOXM1-driven regulatory network in aggressive, therapy-resistant cancers. In silico analyses predict a potential interaction of masitinib with the FOXM1 DNA-binding domain (DBD); however, further experimental validation is required to confirm direct binding.

PMID 42518399
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PubMedFrontiers in medicine2026-07-28

Comparing the efficacy and safety of nafamostat mesylate versus citrate for anticoagulation in continuous renal replacement therapy: a systematic review and meta-analysis.

Zou Zhao Hua ZH, Zhang Ji Quan JQ, Xiang Pei Jun PJ, Chen Xing X et al.

Anticoagulation is pivotal to the successful implementation of continuous renal replacement therapy (CRRT). Systematic comparative studies between nafamostat mesylate (NM) and citrate are scarce. There is currently a lack of evidence-based support for clinical practice. To systematically compare the efficacy and safety of NM versus citrate for anticoagulation in CRRT. We performed a comprehensive literature search in PubMed, Web of Science, Embase, Cochrane Library, China National Knowledge Infrastructure (CNKI), Wanfang Database (Wanfang), China Science and Technology Journal Database (VIP), and China Biological Medicine Database (CBM). Two researchers conducted literature screening, data extraction, and quality assessment using standardized procedures and double-blinded methods. Statistical analyses were performed using Review Manager V.5.4 and STATA 15.1. Statistical heterogeneity among studies was quantified using the Chi-square and I-square tests, and publication bias was evaluated using Egger's test and funnel plots. A total of 18 studies involving 2,247 CRRT patient episodes were included. The meta-analysis showed no significant differences in filter lifespan or clotting events between NM and citrate (MD = -0.11, 95%CI: -1.87 to 1.65, p = 0.90; RR = 0.63, 95%CI: 0.25-1.59, p = 0.33). NM reduced the risk of bleeding events compared with citrate (RR = 0.54, 95%CI: 0.36-0.82, p = 0.003), subgroup analyses showed that NM was associated with a lower risk of bleeding events in high-risk bleeding, low-dose NM, and randomized controlled trials (RCTs) subgroups (RR = 0.47, 95%CI: 0.25-0.88, p = 0.02; RR = 0.39, 95%CI: 0.23-0.66, p < 0.001; RR = 0.21, 95%CI: 0.07-0.66, p = 0.007). No significant differences were found between NM and citrate in platelet (PLT), activated partial thromboplastin time (APTT), or prothrombin time (PT) (MD = 0.88, 95%CI: -5.83 to 7.59, p = 0.80; MD = -0.42, 95%CI: -2.74 to 1.91, p = 0.73; MD =-0.38, 95%CI: -1.45 to 0.68, p = 0.48). NM suggests anticoagulant efficacy comparable to citrate in CRRT, with a lower risk of bleeding, particularly in high bleeding risk situations, among patients receiving low-dose NM. For CRRT patients with contraindications to citrate or high bleeding risk, NM may be an anticoagulant alternative that combines efficacy with safety. The overall certainty of the evidence from this study is low to very low; further multi-center, large-sample, high-quality RCTs are required to validate these findings. https://www.crd.york.ac.uk/PROSPERO/view/CRD420251182609, identifier CRD420251182609.

PMID 42519780
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PubMedMetabolites2026-07-27

Identification and Validation of a Lipid Metabolism-Related Gene Signature for Predicting Prognosis and Immunotherapy Response in Oral Squamous Cell Carcinoma.

Xie Yu Y, Chen Ziying Z, Chen Zhen Z, Yang Yiming Y

Background/Objectives: Lipid metabolism plays a critical role in tumor progression and immunotherapy efficacy in oral squamous cell carcinoma (OSCC). However, clinically applicable lipid metabolism-based models for predicting prognosis and immunotherapy response remain limited. This study aimed to develop and validate such a model in OSCC. Methods: Using transcriptomic data of OSCC from the TCGA database and a set of lipid metabolism-related genes (LMRGs), we constructed an LMRG-based risk score model via LASSO regression to predict patient survival. This model was subsequently validated using the independent GEO dataset GSE41613. Results: Patients in the high-risk group exhibited significantly poorer overall survival than those in the low-risk group (training cohort: p < 0.0001; validation cohort: p = 0.0086). We also developed a nomogram incorporating the risk score and clinical characteristics, and the risk score was identified as an independent prognostic factor for OSCC patients. Furthermore, the risk score was significantly associated with the tumor immune microenvironment; samples with a lower risk score showed elevated CD8+ T cell infiltration and a better response to immunotherapy. Additionally, the high-risk group exhibited an increased tumor mutation burden and resistance to most chemotherapeutic agents. Notably, several drugs (e.g., obatoclax mesylate) showed significant efficacy in the high-risk group, representing promising therapeutic candidates. Conclusions: This study reveals that the LMRG signature could serve as a valuable tool for prognosis assessment, risk stratification, and therapy guidance in OSCC.

PMID 42506409
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PubMedHospital pharmacy2026-07-25

Artificial Intelligence and Large Language Models as Decision-Support Tools in Hospital Compounding Pharmacy: A Proof-of-Concept Study.

Castellana Eleonora E, Chiappetta Maria Rachele MR

To evaluate the efficiency and reliability of a large language model (LLM) as a decision-support tool in hospital compounding pharmacy for pediatric extemporaneous preparations requiring assessment of drug crushability, regulatory compliance, and formulation feasibility. A proof-of-concept study compared a structured LLM-assisted workflow with the traditional manual information retrieval process in a hospital pharmacy setting. The LLM (Claude Sonnet 4.6) was configured with a standardized prompt to extract and consolidate data from multiple authoritative sources: the Friuli Venezia Giulia "Do Not Crush" list, the Italian Medicines Agency (AIFA) database for Summary of Product Characteristics (SmPC), AIFA Law 648/96 off-label use lists, and the Stabilis database for oral liquid formulation stability. Two representative drugs, propranolol hydrochloride and imatinib mesylate, were analyzed. For each drug, the model generated a structured output including crushability, regulatory information, off-label status, and extemporaneous formulation data. The same queries were manually performed by an experienced hospital pharmacist. Primary outcome was information retrieval time; secondary outcomes included completeness and accuracy. The LLM-assisted workflow reduced retrieval time to less than 2 minutes per drug (mean 1 minute 45 seconds), compared with a mean of 20 minutes (range 15-25 minutes) for the manual process, plus an additional 5 to 10 minutes for transcription. Output completeness was 100%, with all predefined fields correctly populated. The model accurately classified drug crushability and correctly identified Law 648/96 regulatory status. For propranolol, the system identified crushability, pediatric off-label authorization, and SyrSpend-based formulations with stability data of up to 146 days at room temperature. For imatinib, the model highlighted cytotoxic handling precautions, identified the absence of SyrSpend formulations, and retrieved alternative formulation stability data (30 days refrigerated). A properly configured LLM can function as an effective decision-support tool in hospital compounding pharmacy, improving efficiency while maintaining high standards of completeness, accuracy, and regulatory compliance. These preliminary results support further investigation into the integration of the LLM system into routine pediatric galenical preparation practice.

PMID 42500259
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PubMedSouth Dakota medicine : the journal of the South Dakota State Medical Association2026-07-22

Epinephrine is Safe in Digital Anesthesia: Debunking the Myth of Finger Necrosis and Correcting Persistent Misinformation in Medical Education.

Van Bockern Ben B, Wilde Emily E, Person Lacey L, Tessendorf Cole D CD et al.

The application of epinephrine in digit procedures has historically been a subject of debate in medical education. Trainees are often advised to avoid its use in fingers, toes, and other terminal areas due to concerns about tissue ischemia and necrosis. However, numerous studies demonstrate that, when used at appropriate concentrations, epinephrine can be safely administered in these regions, challenging long standing misconceptions. The belief that epinephrine causes digital necrosis stems from outdated reports from the early to mid-20th century, many of which involved procaine or cocaine-anesthetics with inherent vasoconstrictive properties that may have compounded the effects of epinephrine. Additionally, procaine alone has been shown to impair tissue viability, likely contributing to observed necrosis. Some case reports of digital necrosis did not involve epinephrine at all, suggesting alternative causes. Despite this, cautious use of epinephrine in digital anesthesia has been incorporated into contemporary medical education. Many reputable textbooks, journals, and online learning resources continue to advise caution against the use of epinephrine in digits, even in light of extensive research suggesting otherwise. When used at an appropriate concentration (1:100,000) alongside an appropriate reversal agent such as phentolamine, epinephrine in the digits has been demonstrated to be safe, with very few reports of necrosis. The use of epinephrine in hand procedures aligns with current best practices and should not be viewed as controversial. Bridging the gap between evidence and education is essential for training clinicians who are confident, competent, and guided by up-to-date, evidence-based practices.

PMID 42485367
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