预约演示

更新于：2025-09-13

Iloperidone

伊潘立酮

更新于：2025-09-13

概要

基本信息

药物类型

小分子化药

别名

1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone、4'-(3-(4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino)propoxy)-3'-methoxyacetophenone、Fanaptum

+ [10]

靶点

5-HT2A receptor x D2 receptor

作用方式

拮抗剂

作用机制

5-HT2A receptor拮抗剂(5-羟色胺2A受体拮抗剂)、D2 receptor拮抗剂(多巴胺D2受体拮抗剂)

治疗领域

其他疾病神经系统疾病

在研适应症

躁郁症1型躁狂精神分裂症

非在研适应症

急性精神分裂症情绪易怒原发性肥大性骨关节病+ [3]

原研机构

Novartis Pharma AG

在研机构

Vanda Pharmaceuticals, Inc.

Novartis AG

Probiomed SA de CV

非在研机构

Novartis Pharmaceuticals Corp.

权益机构

Novartis AG

Vanda Pharmaceuticals, Inc.Aventis SA

+ [1]

最高研发阶段批准上市

首次获批日期

美国 (2009-05-06),

精神分裂症

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C24H27FN2O4

InChIKeyXMXHEBAFVSFQEX-UHFFFAOYSA-N

CAS号133454-47-4

关联

项与伊潘立酮相关的临床试验

NCT07090161

/ Not yet recruiting临床2期

A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Iloperidone for the Treatment of Participants With Uncontrolled Hypertension

A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Iloperidone for the Treatment of Participants with Uncontrolled Hypertension

开始日期2025-07-28

申办/合作机构

Vanda Pharmaceuticals, Inc.

NCT06961968

/ Recruiting临床3期

A Multicenter, Double-Blind, Randomized Withdrawal Study in Patients With Schizophrenia Receiving Either Iloperidone Long-Acting Injection (LAI) or Placebo Injection

The purpose of this research is to evaluate the efficacy of dosing iloperidone long-acting injection (LAI) compared to placebo in preventing the exacerbation of symptoms in patients with schizophrenia.

开始日期2025-05-14

申办/合作机构

Vanda Pharmaceuticals, Inc.

NCT06494397

/ Not yet recruiting临床1期

Crossover Bioequivalence Study of 12 mg VHX-896 and Iloperidone Tablets Under Steady-State Conditions

Study to compare the pharmacokinetics and pharmacodynamics of VHX-896 and iloperidone and evaluate the safety and tolerability of VHX-896 and iloperidone in patients with schizophrenia or bipolar I disorder under steady state conditions.

开始日期2024-07-01

申办/合作机构

Vanda Pharmaceuticals, Inc.

100 项与伊潘立酮相关的临床结果

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100 项与伊潘立酮相关的转化医学

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100 项与伊潘立酮相关的专利（医药）

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380

项与伊潘立酮相关的文献（医药）

2025-10-01·CNS DRUGS

Antipsychotic-Related Prolactin Changes: A Systematic Review and Dose–Response Meta-analysis

Review

作者: Wu, Hui ; Correll, Christoph U ; Leucht, Stefan ; Qin, Mengchang ; Lin, Xiao ; Siafis, Spyridon ; Schneider-Thoma, Johannes ; Tian, Jing

BACKGROUND:

Prolactin increase is a common and potentially problematic adverse event of antipsychotics. We aimed to discover the relationship between antipsychotic doses and changes in prolactin levels.

OBJECTIVE:

To examine the relationship between antipsychotic doses and changes in prolactin levels in adults with acutely exacerbated schizophrenia.

METHODS:

We searched the Cochrane Schizophrenia Group register (last search 26 July 2024) and previous reviews for fixed-dose, randomized controlled trials (RCTs) that investigated monotherapy of 21 antipsychotics in adults with acutely exacerbated schizophrenia. The primary outcome was mean prolactin change from baseline to study endpoint adopting mean differences (MD) in ng/mL as the effect size measure. The dose-response curves were estimated by conducting random-effects dose-response meta-analyses using the restricted cubic spline method.

RESULTS:

Among 165 eligible studies, 68 studies with 238 dose arms (23,128 participants, 35% female) reported on prolactin and were meta-analyzed. Of these, 94% lasted ≤ 3 months, and 90% of the studies used oral formulations. Participants in one study experienced their first episode, while all other studies also included multiepisode participants. The dose-response curves indicated that with aripiprazole, higher doses were significantly associated with lower prolactin levels than lower doses. Brexpiprazole, cariprazine, lumateperone, and quetiapine carried negligible risks for prolactin increase across examined doses. During treatment with most other antipsychotics, i.e., asenapine, haloperidol, iloperidone, lurasidone, olanzapine, paliperidone, risperidone, and ziprasidone, prolactin levels rose with increasing doses and then continued to increase or plateaued. The shape of the dose-response curves was similar in males and females, with generally larger amplitudes of the curves in females.

CONCLUSIONS:

The prolactin-increasing property varies among antipsychotics, is dose-related, and is greater in females. These findings in adults with acutely exacerbated schizophrenia can help clinicians titrate and adapt antipsychotic doses and consider patients' sex in treatment decisions. The protocol was registered in the International Prospective Register of Systematic Reviews (PROSPERO); registration no. CRD42020181467.

2025-10-01·CNS DRUGS

Strategies for Switching between Oral Postsynaptic Antidopaminergic Antipsychotics in Patients with Schizophrenia: A Systematic Review

Review

作者: Correll, Christoph U

BACKGROUND:

Antipsychotic switching is common in the treatment of schizophrenia. Pharmacokinetic and pharmacodynamic properties of antipsychotics can inform switch strategies, as switching from shorter to longer half-life antipsychotics and switching from more antagonistic to less antagonistic or partial agonist agents at dopaminergic, histaminergic, and cholinergic receptors can lead to withdrawal or rebound symptoms, potentially complicating switch results. This systematic literature review of studies investigated switching strategies between oral antipsychotics. Pharmacokinetic and pharmacodynamic characteristics of antipsychotics that can influence switch outcomes were also extracted from publications and prescribing information.

METHODS:

MEDLINE, Embase, Cochrane Central Register of Controlled Trials, and PubMed databases were queried (last search 13 May 2024) for articles published from 1 June 2010 to 1 April 2024, with keywords (schizophr* OR schizoaff*) AND (antipsychotic*) AND (switch*). Randomized controlled trials, open-label studies, meta-analyses, and reviews of oral antipsychotic switching were included. Records were excluded if they investigated a disease other than schizophrenia or schizoaffective disorder or focused on long-acting injectable or non-approved antipsychotics. Data on switch strategies investigated and study outcomes were manually extracted from randomized controlled trials and open-label switch studies of oral antipsychotics in schizophrenia or schizoaffective disorder. Meta-analyses and review articles were summarized. There was no assessment for risk of bias or specific method to synthesize results.

RESULTS:

Of the 579 records identified during the systematic review, 80 articles investigated switching of oral antipsychotics in adult patients with schizophrenia, including 58 randomized and non-randomized studies (9 of which investigated ≥ 1 antipsychotic) and 22 review articles or meta-analyses. The antipsychotics investigated during this period were: aripiprazole (studies = 18); paliperidone, ziprasidone, olanzapine, and risperidone (studies = 7 each); brexpiprazole, clozapine and lurasidone (studies = 4 each); amisulpride, (studies = 3); quetiapine and iloperidone (studies = 2 each); and asenapine and lumateperone (1 study each). Most studies that reported a switch method employed cross-titration switching (studies = 39; 69.6%), while abrupt switching (studies = 10; 17.9%) and switching at investigator's discretion (studies = 7; 12.5%) were rare. A total of 24 studies (N = 3440 patients) had statistical comparisons between treatment groups, but few studies specifically statistically compared outcomes between different switch strategies (1 trial each for aripiprazole, clozapine, iloperidone, and ziprasidone; N = 666 patients), with mixed outcomes. Frequencies of sedative rescue treatments, which could have attenuated potential withdrawal symptoms, were rarely disclosed.

CONCLUSIONS:

Despite the importance and frequency of antipsychotic switching, few studies have specifically investigated outcomes of different switch strategies. General clinical preference appears to utilize gradual switching approaches to avoid potential rebound symptoms. Future research with current and emerging antipsychotics is needed, especially for switching between antipsychotics with different receptor profiles and for switches that are potentially vulnerable to rebound and withdrawal symptoms.

2025-09-01·ANNALS OF PHARMACOTHERAPY

An Evaluation of Iloperidone for Mania in Bipolar I Disorder

Review

作者: Caskey, Kelen ; Nelson, Leigh Anne

Objective::

To review the efficacy of iloperidone for mania associated with bipolar I disorder and discuss its safety profile (eg, QTc prolongation, orthostatic hypotension, and metabolic adverse effects).

Data sources::

Literature was identified using PubMed (1966-September 2024), OVID (1984-November 2024), and clinicaltrials.gov. Search terms included iloperidone, bipolar disorder, and mania.

Study selection and data extraction::

The study included trials evaluating iloperidone for treating bipolar mania.

Data synthesis::

In one phase 3 study, iloperidone demonstrated significant improvement in mania symptoms at day 28 on all primary (ie, Young Mania Rating Scale) and secondary outcomes (Clinical Global Impression-Severity/Change scales) compared to placebo. Iloperidone was well tolerated, with tachycardia, dizziness, dry mouth, alanine aminotransferase elevation, nasal congestion, increased weight, and somnolence reported as common adverse effects.

Relevance to patient care and clinical practice in comparison to existing drugs::

Since there are no head-to-head studies comparing iloperidone with other second-generation antipsychotics for bipolar mania, other treatment considerations drive medication selection. Iloperidone is unavailable in a generic formulation; thus, its use will be associated with higher costs. It is dosed twice daily, which may negatively impact adherence. Iloperidone is associated with a moderate risk of QTc prolongation, metabolic adverse effects, and orthostatic hypotension, which will limit its use in certain patient populations. QTc prolongation is dose related, so drug interactions involving CYP2D6 and CYP3A4 inhibition can have serious consequences.

Conclusion::

In the pivotal trial, iloperidone was effective in treating adults with an acute manic or mixed episode associated with bipolar I disorder and was safe and well tolerated.

项与伊潘立酮相关的新闻（医药）

2025-05-07

·PRNewswire

Vanda Pharmaceuticals Reports First Quarter 2025 Financial Results

Fanapt® Q1 2025 total prescriptions (TRx) increased 14% compared to Q1 2024 Fanapt® Q1 2025 new to brand prescriptions (NBRx) increased nearly threefold compared to Q1 2024 Bysanti™ (milsaperidone) NDA for bipolar I disorder and schizophrenia accepted for filing; PDUFA target action date of February 21, 2026 Tradipitant NDA for motion sickness accepted for filing; PDUFA target action date of December 30, 2025 Imsidolimab BLA in generalized pustular psoriasis expected to be submitted in 2025 WASHINGTON, May 7, 2025 /PRNewswire/ -- Vanda Pharmaceuticals Inc. (Vanda) (Nasdaq: VNDA) today announced financial and operational results for the first quarter ended March 31, 2025. Continue Reading Fanapt® TRx and NBRx "Vanda has entered a new growth phase with multiple commercialized products and a rich innovative pipeline. Fanapt commercial growth has accelerated, reaching multi-year highs, with weekly prescriptions surpassing 2,000 at the end of April as an increasing number of prescribers are adding Fanapt to their therapeutic armamentarium," said Mihael H. Polymeropoulos, M.D., Vanda's President, CEO and Chairman of the Board. "Our recent new drug application filings for tradipitant and Bysanti are a testament to our productive research and development pipeline. The addition of imsidolimab alongside Ponvory establishes an anti-inflammatory franchise that we believe has significant growth potential. These accomplishments have been possible because of our talented employees, who for the first time surpassed 400 in number, a 22-year high." Financial Highlights Total net product sales from Fanapt®, HETLIOZ® and PONVORY® were $50.0 million in the first quarter of 2025, a 5% increase compared to $47.5 million in the first quarter of 2024. Fanapt® net product sales were $23.5 million in the first quarter of 2025, a 14% increase compared to $20.6 million in the first quarter of 2024. HETLIOZ® net product sales were $20.9 million in the first quarter of 2025, a 4% increase compared to $20.1 million in the first quarter of 2024. PONVORY® net product sales were $5.6 million in the first quarter of 2025, a decrease of 18% compared to $6.8 million in the first quarter of 2024. Net loss was $29.5 million in the first quarter of 2025 compared to net loss of $4.1 million in the first quarter of 2024. The net loss in the first quarter of 2025 reflects expenses associated with the payment of $15.0 million related to the exclusive, global license agreement with AnaptysBio, Inc. (Anaptys) for the development and commercialization of imsidolimab and increased commercial activities. Cash, cash equivalents and marketable securities (Cash) was $340.9 million as of March 31, 2025, representing a decrease to Cash of $33.7 million compared to December 31, 2024. The decrease to Cash reflects the payment of $15.0 million during the first quarter of 2025 related to the exclusive, global license agreement with Anaptys for the development and commercialization of imsidolimab. Key Operational Highlights – Commercial Fanapt® (iloperidone) Fanapt® was approved in the second quarter of 2024 for the acute treatment of bipolar I disorder. Vanda initiated the commercial launch of Fanapt® in this indication in the third quarter of 2024. In the first quarter of 2025, as compared to the first quarter of 2024, total prescriptions (TRx)1 increased by approximately 14% and Fanapt® net product sales increased by 14%. Additionally, new patient starts, as reflected by new to brand prescriptions (NBRx),1 increased by nearly threefold in the same period. Fanapt® total prescriptions (TRx) for the week of April 25, 2025 reached the milestone of 2,000, making Fanapt® one of the fastest growing atypical antipsychotics.1 Vanda has also announced an expansion of its psychiatry sales force to approximately 300 representatives. HETLIOZ® (tasimelteon) Through the first quarter of 2025, HETLIOZ® continues to retain the largest portion of market share despite generic competition for over two years.2 PONVORY® (ponesimod) Vanda initiated the commercial launch of PONVORY® for the treatment of relapsing forms of multiple sclerosis in the third quarter of 2024. In April 2025, new patient prescriptions reached a new record high since the initiation of Vanda's commercial launch. Vanda has re-enforced the PONVORY® sales leadership team and announced an expansion of its PONVORY® sales force to approximately 40 representatives. Key Operational Highlights – Regulatory & Clinical Development Key Regulatory Milestones Tradipitant New Drug Application (NDA) for motion sickness accepted for filing by the U.S. Food and Drug Administration (FDA) with a Prescription Drug User Fee Act (PDUFA) target action date of December 30, 2025. Fanapt® Marketing Authorization Application (MAA) for bipolar I disorder and schizophrenia submitted to the European Medicines Agency (EMA) in Q4 2024. HETLIOZ® MAA in Smith-Magenis syndrome (SMS) submitted to the EMA in Q4 2024. Bysanti™ NDA for bipolar I disorder and schizophrenia accepted for filing by the FDA with a PDUFA target action date of February 21, 2026. Imsidolimab Biologics License Application (BLA) in generalized pustular psoriasis (GPP) expected to be submitted to the FDA in 2025. Key Clinical Highlights Fanapt® (iloperidone) Schizophrenia: A Phase III program for the long acting injectable (LAI) formulation of Fanapt® in the treatment of schizophrenia in relapse prevention is ongoing. Hypertension: Vanda initiated a study of the Fanapt® LAI as a once-a-month injectable for uncontrolled hypertension and plans to begin enrolling patients soon. Bysanti™ (milsaperidone) The NDA for Bysanti™ for the acute treatment of bipolar I disorder and the treatment of schizophrenia was accepted for filing by the FDA with a PDUFA target action date of February 21, 2026. Exclusivity for Bysanti™, including pending patent applications, could extend into the 2040s. Bysanti™ is a new chemical entity, which was initially identified as an active metabolite of iloperidone. Vanda discovered that milsaperidone, when administered orally, quickly interconverts to iloperidone. In clinical studies, milsaperidone and iloperidone have been shown to be bioequivalent at both low and high doses, administered both in single and multiple dose studies. The results of these clinical studies will be presented in late May, at the 2025 American Society of Clinical Psychopharmacology annual meeting in Scottsdale, Arizona. The Bysanti™ Phase III clinical study for use as a once-daily adjunctive treatment for major depressive disorder (MDD) is ongoing. Results are expected in 2026. HETLIOZ® (tasimelteon) HETLIOZ® clinical programs in pediatric insomnia and delayed sleep phase disorder (DSPD) are ongoing. Vanda's MAA for HETLIOZ® and HETLIOZ LQ® for SMS is pending with the EMA. PONVORY® (ponesimod) Investigational New Drug (IND) applications for PONVORY® in the treatments of psoriasis and ulcerative colitis were accepted by the FDA in the fourth quarter of 2024. Tradipitant The NDA for tradipitant for the treatment of motion sickness was accepted for filing by the FDA with a PDUFA target action date of December 30, 2025. In the fourth quarter of 2024, Vanda initiated a clinical trial to study tradipitant in the prevention of vomiting induced by a GLP-1 analog, Wegovy (semaglutide). Results are expected in the third quarter of 2025. Imsidolimab In February 2025, Vanda announced it entered into an exclusive, global license agreement with Anaptys for the development and commercialization of imsidolimab (IL-36R antagonist mAb). A BLA for GPP is expected to be submitted to the FDA in 2025. Early-Stage Program Highlights VQW-765, an alpha-7 nicotinic acetylcholine receptor partial agonist, is currently in clinical development for the treatment of acute performance anxiety in social situations. Vanda expects to initiate the Phase III program in 2025. The IND application for VCA-894A in the treatment of Charcot-Marie-Tooth disease, axonal, type 2S (CMT2S), an inherited peripheral neuropathy for which there is no available treatment, was accepted by the FDA in 2024. Previously in 2023, VCA-894A was granted Orphan Drug Designation for the same indication. The Phase I clinical study for VCA-894A expects to enroll the patient by mid-2025. GAAP Financial Results Net loss was $29.5 million in the first quarter of 2025 compared to net loss of $4.1 million in the first quarter of 2024. Diluted net loss per share was $0.50 in the first quarter of 2025 compared to diluted net loss per share of $0.07 in the first quarter of 2024. 2025 Financial Guidance Vanda is reiterating its 2025 total revenues guidance and updating its 2025 financial guidance to include year-end 2025 Cash. Vanda expects to achieve the following financial objectives in 2025: Conference Call Vanda has scheduled a conference call for today, Wednesday, May 7, 2025, at 4:30 PM ET. During the call, Vanda's management will discuss the first quarter 2025 financial results and other corporate activities. Investors can call 1-800-715-9871 (domestic) or 1-646-307-1963 (international) and use passcode number 9941754. A replay of the call will be available on Wednesday, May 7, 2025, beginning at 8:30 PM ET and will be accessible until Wednesday, May 14, 2025 at 11:59 PM ET. The replay call-in number is 1-800-770-2030 for domestic callers and 1-609-800-9909 for international callers. The passcode number is 9941754. The conference call will be broadcast simultaneously on Vanda's website, . Investors should click on the Investors tab and are advised to go to the website at least 15 minutes early to register, download, and install any necessary software or presentations. The call will also be archived on Vanda's website for a period of 30 days. References IQVIA Prescription Data Based on blended data analysis About Vanda Pharmaceuticals Inc. Vanda is a leading global biopharmaceutical company focused on the development and commercialization of innovative therapies to address high unmet medical needs and improve the lives of patients. For more on Vanda Pharmaceuticals Inc., please visit and follow us on X @vandapharma. CAUTIONARY NOTE REGARDING FORWARD LOOKING STATEMENTS Various statements in this press release, including, but not limited to, the guidance provided under "2025 Financial Guidance" above and statements regarding the growth potential of Vanda's anti-inflammatory franchise; Vanda's plans for pursuit of FDA approval of Bysanti™ for the acute treatment of bipolar I disorder and the treatment of schizophrenia, tradipitant for the treatment of motion sickness, and imsidolimab for the treatment of GPP, and the related timelines; Vanda's plans for pursuit of EMA approval of Fanapt® for the treatment of bipolar I disorder and schizophrenia and HETLIOZ® and HETLIOZ LQ® for the treatment of SMS; Vanda's clinical development plans and expected timelines for Fanapt® LAI as a once-a-month injectable for uncontrolled hypertension, Bysanti™ for the treatment of MDD, VQW-765 for the treatment of acute performance anxiety in social situations, and VCA-894A for the treatment of CMT2S; the expected timing of the results of the tradipitant clinical trial for the prevention of vomiting induced by Wegovy; and the potential to extend patent exclusivity for Bysanti™ into the 2040s are "forward-looking statements" under the securities laws. All statements other than statements of historical fact are statements that could be deemed forward-looking statements. Forward-looking statements are based upon current expectations and assumptions that involve risks, changes in circumstances and uncertainties. Important factors that could cause actual results to differ materially from those reflected in Vanda's forward-looking statements include, among others, Vanda's ability to continue to grow its business; Vanda's ability to obtain regulatory approval and execute a successful commercial launch of imsidolimab, and increase PONVORY® revenue; the FDA's ability to complete its reviews of, and reach decisions with respect to, the NDAs for Bysanti™ and tradipitant by their respective PDUFA target action dates; Vanda's ability to complete and submit the BLA for imsidolimab in 2025; Vanda's ability to obtain EMA approval of the MAAs for Fanapt® and HETLIOZ® and HETLIOZ LQ®, Vanda's ability to begin enrolling patients in the Fanapt® LAI study within the specified timeframe; Vanda's ability to complete the Phase III clinical study for Bysanti™ for MDD and receive results in 2026; Vanda's ability to complete the clinical trial of tradipitant for the prevention of vomiting induced by Wegovy and receive results in the third quarter of 2025; Vanda's ability to initiate the Phase III program for VQW-765 in 2025; Vanda's ability to enroll the CMT2S patient in the Phase I clinical study for VCA-894A by mid-2025; and Vanda's ability to satisfy the conditions necessary to extend Bysanti™'s patent exclusivity into the 2040s. Therefore, no assurance can be given that the results or developments anticipated by Vanda will be realized or, even if substantially realized, that they will have the expected consequences to, or effects on, Vanda. Forward-looking statements in this press release should be evaluated together with the various risks and uncertainties that affect Vanda's business and market, particularly those identified in the "Cautionary Note Regarding Forward-Looking Statements", "Risk Factors" and "Management's Discussion and Analysis of Financial Condition and Results of Operations" sections of Vanda's most recent Annual Report on Form 10-K, as updated by Vanda's subsequent Quarterly Reports on Form 10-Q, Current Reports on Form 8-K and other filings with the U.S. Securities and Exchange Commission, which are available at . All written and verbal forward-looking statements attributable to Vanda or any person acting on its behalf are expressly qualified in their entirety by the cautionary statements contained or referred to herein. Vanda cautions investors not to rely too heavily on the forward-looking statements Vanda makes or that are made on its behalf. The information in this press release is provided only as of the date of this press release, and Vanda undertakes no obligation, and specifically declines any obligation, to update or revise publicly any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. Corporate Contact: Kevin Moran Senior Vice President, Chief Financial Officer and Treasurer Vanda Pharmaceuticals Inc. 202-734-3400 [email protected] Jim Golden / Jack Kelleher / Dan Moore Collected Strategies [email protected] Follow us on X @vandapharma SOURCE Vanda Pharmaceuticals Inc. 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临床1期引进/卖出上市批准临床3期申请上市

2025-05-05

·药明康德

潜在“first-in-class”免疫疗法组合显著延长癌症患者生命；创新抗体获FDA突破性疗法认定……

潜在“first-in-class”LAG-3组合疗法显著延长癌症患者生命Immutep公司今日宣布，其2b期临床试验TACTI-003（KEYNOTE-C34）患者队列B取得积极结果：中位总生存期（OS）达17.6个月。该队列旨在评估eftilagimod alfa（efti）联合默沙东（MSD）的抗PD-1疗法Keytruda（pembrolizumab）作为复发/转移性头颈部鳞状细胞癌（HNSCC）患者一线治疗方案的效果，受试者为PD-L1表达综合阳性评分（CPS）低于1的人群。截至2025年3月31日，评估人群（N=31）的成熟中位OS为17.6个月，显著优于当前标准治疗方案在CPS＜1患者中的历史数据（10.7~11.3个月）。LAG-3蛋白能够调控T淋巴细胞和抗原呈现细胞（APCs）的信号通路，在适应性免疫反应中起到重要作用。Efti是一种潜在“first-in-class”可溶性LAG-3融合蛋白。通过与APC表面的主要组织相容性复合体II（MHC II）相结合，能够激活APCs，这会激活和增殖CD8阳性细胞毒性T细胞、CD4阳性辅助性T细胞、树突状细胞、NK细胞和单核细胞，提升患者对癌症抗原的免疫反应。此外，Efti还能上调IFN-γ和CXCL10等关键生物分子的表达，进一步增强免疫系统对抗癌症的能力。Keytruda通过阻断具有免疫抑制功能的PD-1信号通路，增强T细胞的抗癌免疫反应。两种疗法具有互补的作用机制。别构调节胰岛素信号通路，创新抗体获FDA突破性疗法认定Rezolute公司今日宣布，美国FDA已授予其在研疗法ersodetug突破性疗法认定，用于治疗肿瘤性高胰岛素血症（HI）所导致低血糖。Ersodetug是一种全人源化单克隆抗体，可与肝脏、脂肪和肌肉中胰岛素受体上的独特别构位点结合。该抗体通过调节胰岛素的结合、信号和活性来抵消体内胰岛素升高的影响，从而将葡萄糖水平维持在正常范围内。由于ersodetug作用于胰腺下游，因此有潜力成为普适性疗法，用于治疗因先天性或获得性HI所致的低血糖。这一突破性疗法认定的授予是基于ersodetug在整个临床开发项目中的试验数据，以及其治疗机制在肿瘤性HI中的适用性。此前发表的2b期临床试验结果显示，ersodetug能显著改善先天性HI患者的低血糖，且伴有良好的安全性和耐受性。Rezolute计划于2025年年中启动针对肿瘤性HI患者的注册性研究，预计将在2026年下半年公布顶线结果。治疗I型双相情感障碍，FDA接受创新小分子疗法新药申请Vanda Pharmaceuticals今日宣布，美国FDA已受理其为在研疗法Bysanti（milsaperidone）递交的新药申请（NDA），用于治疗1型双相情感障碍（BP-I）和精神分裂症。FDA预计在2026年2月21日前完成审评。Bysanti是一种新化学实体。Vanda发现，经口服给药后，milsaperidone可迅速转化为iloperidone（一种已上市抗精神病药物）。临床研究显示，在低剂量和高剂量下，无论是单次给药还是多次给药，milsaperidone与iloperidone的生物等效性均已被证实。Bysanti在治疗BP-I相关的躁狂或混合发作，以及精神分裂症方面的疗效与安全性，获得了iloperidone说明书中所列举的临床研究的支持，包括两项急性精神分裂症发作研究、一项针对BP-I躁狂或混合发作的研究，以及一项精神分裂症复发预防研究。此外，Bysanti的安全性也得到了iloperidone临床研究中数千名患者数据的支持。Milsaperidone独特的物理和化学性质使其适合在未来开发为长效注射剂型。Bysanti属于非典型抗精神病药物类别，显示出对α1肾上腺素能受体的高亲和力，同时也作用于某些5-羟色胺和多巴胺受体，这些受体被认为与其治疗效应密切相关。参考资料：[1] Vanda Announces Bysanti™ NDA Filing; FDA Decision Expected in Early 2026. Retrieved May 5, 2025, from https://www.prnewswire.com/news-releases/vanda-announces-bysanti-nda-filing-fda-decision-expected-in-early-2026-302445753.html[2] Immutep’s Efti in Combination with KEYTRUDA® (pembrolizumab) Drives Strong Overall Survival in Head and Neck Cancer with CPS <1. Retrieved May 5, 2025, from https://www.immutep.com/detail/immutep-s-efti-in-combination-with-keytruda-r-pembrolizumab-drives-strong-overall-survival-in-head-and-neck-cancer-with-cps-1.html[3] Rezolute Receives Breakthrough Therapy Designation from FDA for Ersodetug in the Treatment of Hypoglycemia Due to Tumor Hyperinsulinism. Retrieved May 5, 2025, from https://www.globenewswire.com/news-release/2025/05/05/3074006/0/en/Rezolute-Receives-Breakthrough-Therapy-Designation-from-FDA-for-Ersodetug-in-the-Treatment-of-Hypoglycemia-Due-to-Tumor-Hyperinsulinism.html免责声明：本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

突破性疗法免疫疗法临床结果临床2期

2025-05-05

·PRNewswire

Vanda Announces Bysanti™ NDA Filing; FDA Decision Expected in Early 2026

WASHINGTON, May 5, 2025 /PRNewswire/ -- Vanda Pharmaceuticals Inc. (Vanda) (Nasdaq: VNDA) today announced that the U.S. Food and Drug Administration (FDA) informed Vanda that the New Drug Application (NDA) for Bysanti™ (milsaperidone) has been filed, and that at this time no potential review issues have been identified. The FDA has set February 21, 2026 as the target date for decision on this application. Bysanti™ is a new chemical entity, which was initially identified as an active metabolite of iloperidone. Vanda has discovered that milsaperidone, when administered orally, quickly interconverts to iloperidone. In clinical studies, milsaperidone and iloperidone have been shown to be bioequivalent at both low and high doses, administered both in single and multiple dose studies. The results of these clinical studies will be presented in late May, at the 2025 American Society of Clinical Psychopharmacology annual meeting in Scottsdale, Arizona. The efficacy and safety of Bysanti™ for the indications of bipolar I manic and mixed episodes and schizophrenia are supported by the clinical studies described on the iloperidone prescribing information. These include two studies in acute episodes of schizophrenia, one study in bipolar I disorder with manic or mixed episodes, and one relapse prevention study in schizophrenia. The safety of Bysanti™ is further supported by data in several thousand patients exposed to iloperidone in clinical studies, as well as the post marketing iloperidone experience, with more than 80,000 patient year exposures. The unique physical and chemical properties of milsaperidone make it amenable to the development of lipid esters that could allow the future development of long acting injectable formulations. Bysanti™ is currently under development in a clinical study as a once-a-day adjunctive treatment of major depressive disorder (MDD) for patients with inadequate response on their current treatment. Results are expected in 2026. Bysanti™ is eligible for 5 year regulatory data exclusivity if approved by the FDA. Current Bysanti™ related patent applications, if issued, would extend into the 2040's. Bysanti™ belongs to the class of atypical antipsychotics showing strong affinity to the alpha 1 adrenergic receptor, in addition to certain serotonin and dopamine receptors that are believed to explain its therapeutic effects. "The extraordinary discovery of bioequivalence to iloperidone, of this novel chemical entity, allows for the efficient development of Bysanti™ and opens new opportunities to further explore additional therapeutic applications of this molecule," said Dr. Mihael Polymeropoulos, Vanda's President, CEO and Chairman of the Board. About Bysanti™ Bysanti™ is a new chemical entity that belongs in the class of atypical antipsychotic drugs. If approved, Bysanti™ could be available for sale in the US in 2026. Bysanti™ is believed to achieve its therapeutic effect by interacting with a host of neurotransmitter receptors in the brain, including the alpha-adrenergic receptor, serotonin receptors and dopamine receptors. Exclusivity, including pending patent applications, could extend into the 2040s. About Vanda Pharmaceuticals Inc. Vanda is a leading global biopharmaceutical company focused on the development and commercialization of innovative therapies to address high unmet medical needs and improve the lives of patients. For more on Vanda Pharmaceuticals Inc., please visit and follow us on X @vandapharma. CAUTIONARY NOTE REGARDING FORWARD LOOKING STATEMENTS Various statements in this press release, including, but not limited to, statements regarding the potential to develop long acting injectable formulations of Bysanti™, the expected timing of the clinical study results for Bysanti™ in MDD, Bysanti™'s mechanism of action, the potential commercial availability of Bysanti™, the potential to extend patent exclusivity for Bysanti™ into the 2040s, the potential to develop additional therapeutic applications for Bysanti™, and the anticipated timing of the completion of the FDA's review of the Bysanti™ NDA are "forward-looking statements" under the securities laws. All statements other than statements of historical fact are statements that could be deemed forward-looking statements. Forward-looking statements are based upon current expectations and assumptions that involve risks, changes in circumstances and uncertainties. Important factors that could cause actual results to differ materially from those reflected in Vanda's forward-looking statements include, among others, Vanda's ability to complete its clinical study in MDD and report results in 2026, Vanda's assumptions regarding how Bysanti™ achieves its therapeutic effect, Vanda's ability to obtain regulatory approval for Bysanti™ for the acute treatment of bipolar I disorder and schizophrenia and initiate its commercial launch in 2026, Vanda's ability to satisfy the conditions necessary to extend Bysanti™'s patent exclusivity into the 2040s, Vanda's ability to identify additional indications for Bysanti™ and the FDA's ability to complete its review of, and reach a decision with respect to, the Bysanti™ NDA by February 21, 2026. Therefore, no assurance can be given that the results or developments anticipated by Vanda will be realized or, even if substantially realized, that they will have the expected consequences to, or effects on, Vanda. Forward-looking statements in this press release should be evaluated together with the various risks and uncertainties that affect Vanda's business and market, particularly those identified in the "Cautionary Note Regarding Forward-Looking Statements", "Risk Factors" and "Management's Discussion and Analysis of Financial Condition and Results of Operations" sections of Vanda's most recent Annual Report on Form 10-K, as updated by Vanda's subsequent Quarterly Reports on Form 10-Q, Current Reports on Form 8-K and other filings with the U.S. Securities and Exchange Commission, which are available at . All written and verbal forward-looking statements attributable to Vanda or any person acting on its behalf are expressly qualified in their entirety by the cautionary statements contained or referred to herein. Vanda cautions investors not to rely too heavily on the forward-looking statements Vanda makes or that are made on its behalf. The information in this press release is provided only as of the date of this press release, and Vanda undertakes no obligation, and specifically declines any obligation, to update or revise publicly any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. Corporate Contact: Kevin Moran Senior Vice President, Chief Financial Officer and Treasurer Vanda Pharmaceuticals Inc. 202-734-3400 [email protected] Jim Golden/Jack Keleher/Dan Moore Collected Strategies [email protected] SOURCE Vanda Pharmaceuticals Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

申请上市

100 项与伊潘立酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02666	伊潘立酮	N05AX14	DB04946

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
躁郁症1型	美国	Vanda Pharmaceuticals, Inc.	2024-04-02
躁狂	美国	Vanda Pharmaceuticals, Inc.	2024-04-02
精神分裂症	美国	Vanda Pharmaceuticals, Inc.	2009-05-06

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
急性精神分裂症	临床3期	美国	Vanda Pharmaceuticals, Inc.	2005-11-18
急性精神分裂症	临床3期	印度	Vanda Pharmaceuticals, Inc.	2005-11-18
原发性肥大性骨关节病	临床2期	美国	Vanda Pharmaceuticals, Inc.	2022-06-01
帕金森病	临床2期	美国	Vanda Pharmaceuticals, Inc.	2022-06-01
情绪易怒	临床2期	美国	Novartis Pharmaceuticals Corp.	2013-07-01
入睡和睡眠障碍	临床2期	美国	Novartis Pharmaceuticals Corp.	2013-07-01
创伤后应激障碍	临床2期	美国	Novartis Pharmaceuticals Corp.	2013-07-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00254202 (CTgov)	临床3期	急性精神分裂症	593	Iloperidone (Iloperidone)	蓋襯顧範選積鑰鏇願衊(鏇簾鑰憲製壓餘艱艱鑰) = 構壓糧壓構衊觸艱繭築鏇窪範顧衊襯願憲顧鹽 (鑰廠糧鹽觸鹹蓋觸網衊, 1.03) 更多	-	2024-12-13
				Ziprasidone (Ziprasidone)	蓋襯顧範選積鑰鏇願衊(鏇簾鑰憲製壓餘艱艱鑰) = 夢夢構衊艱築壓淵蓋夢鏇窪範顧衊襯願憲顧鹽 (鑰廠糧鹽觸鹹蓋觸網衊, 1.44) 更多
NCT04819776 (CTgov)	临床3期	躁狂 \| 躁郁症1型	417	Iloperidone (Iloperidone)	繭鬱鹹餘範憲齋觸顧範(觸選壓獵鹽艱顧糧蓋廠) = 鹹淵觸積餘構膚鏇衊鬱糧鹹網遞築鏇願鏇鹽鹽 (廠選選網鏇廠鏇選鹹鹹, 0.64) 更多	-	2024-04-16
				Iloperidone Placebo (Placebo)	繭鬱鹹餘範憲齋觸顧範(觸選壓獵鹽艱顧糧蓋廠) = 糧膚鬱憲繭製鹽鹹淵艱糧鹹網遞築鏇願鏇鹽鹽 (廠選選網鏇廠鏇選鹹鹹, 0.63) 更多
NCT01291511 (REPRIEVE, CTgov)	临床3期	精神分裂症	635	Iloperidone (Iloperidone)	膚積觸膚淵淵蓋醖鬱淵(簾夢蓋廠鏇窪獵觸繭夢) = 遞廠鹹壓糧糧製襯淵觸夢醖製鹹觸憲糧鏇衊繭 (艱襯廠憲繭醖鏇廠觸獵, 夢願膚糧醖簾鹽顧範繭 ~ 鏇鏇獵繭壓繭願蓋築夢) 更多	-	2023-07-17
				Placebo (Placebo)	膚積觸膚淵淵蓋醖鬱淵(簾夢蓋廠鏇窪獵觸繭夢) = 壓簾獵觸網艱構淵鬱醖夢醖製鹹觸憲糧鏇衊繭 (艱襯廠憲繭醖鏇廠觸獵, 築鹹鏇繭積鑰願鬱壓醖 ~ 繭鏇窪製築遞壓窪壓衊) 更多
NCT01917318 (CTgov)	临床2期	入睡和睡眠障碍 \| 创伤后应激障碍 \| 情绪易怒	1	Placebo+Iloperidone (Iloperidone / Placebo)	鹹範鏇鬱鹹積憲觸鏇鬱(鬱構齋齋壓製衊淵遞淵) = 廠觸鏇觸獵範範夢獵廠鏇壓願製廠鏇遞構醖觸 (鏇製鹽鏇餘簾衊壓淵鬱, 鹹構願襯壓憲艱衊憲觸 ~ 艱遞艱廠獵築襯糧鏇夢) 更多	-	2020-01-31
				Placebo+Iloperidone (Placebo / Iloperidone)	鏇壓鹹顧顧醖廠製鏇廠 = 願齋壓窪築醖憲觸廠衊艱構餘膚鹽壓積製醖顧 (夢淵憲淵膚築顧選鹽憲, 鑰範齋鑰齋齋膚積窪製 ~ 艱積選壓鑰廠壓鹽艱鑰) 更多
NCT01920802 (CTgov)	临床4期	-	31	olanzapine (Olanzapine)	簾餘顧觸範鏇遞願衊醖(蓋鏇廠鹽築蓋夢壓顧蓋) = 網廠遞鏇鏇鹹壓選壓糧網窪簾艱蓋醖鹹淵憲鹹 (積齋積獵衊鑰憲餘觸廠, 1.0) 更多	-	2017-03-20
				iloperidone (Iloperidone)	簾餘顧觸範鏇遞願衊醖(蓋鏇廠鹽築蓋夢壓顧蓋) = 鬱觸顧鏇獵觸鏇膚鏇構網窪簾艱蓋醖鹹淵憲鹹 (積齋積獵衊鑰憲餘觸廠, 0.7) 更多
NCT01291511 (REPRIEVE, Pubmed \| CNS Drugs) 人工标引	临床3期	精神分裂症	303	Iloperidone	壓網簾願製襯襯網鑰積(製膚憲簾蓋膚衊選鬱窪) = 鹹網蓋獵鑰遞積糧糧積網築糧齋鏇鹹觸壓範糧 (遞範鬱糧簾願夢鑰鏇齋 ) 更多	积极	2016-08-01
				Placebo	壓網簾願製襯襯網鑰積(製膚憲簾蓋膚衊選鬱窪) = 鏇艱積蓋鹹齋憲齋艱鑰網築糧齋鏇鹹觸壓範糧 (遞範鬱糧簾願夢鑰鏇齋 ) 更多
NCT01929889 (CTgov)	临床4期	分裂情感性障碍 \| 精神分裂症	19	Iloperidone	壓範願製築顧選艱範窪(鑰壓鑰選簾鏇選簾鑰簾) = 鬱願憲壓積糧壓餘鏇構遞鹹鹽鬱襯遞糧繭憲顧 (艱壓網獵構鹽齋蓋襯願, 3.742) 更多	-	2015-07-10
NCT01207414 (i-FANS, CTgov)	临床4期	精神分裂症	501	iloperidone (Iloperidone Gradual Switch)	襯築鬱網鑰築選淵壓範(鹽製築顧糧築鏇獵積顧) = 醖鹽醖齋壓廠淵顧夢淵觸夢積積積簾鹹衊鬱獵 (積蓋鏇鹹願淵廠憲膚鹹, 1.1244) 更多	-	2013-03-15
				iloperidone (Iloperidone Immediate Switch)	襯築鬱網鑰築選淵壓範(鹽製築顧糧築鏇獵積顧) = 膚窪繭淵獵夢鏇襯艱願觸夢積積積簾鹹衊鬱獵 (積蓋鏇鹹願淵廠憲膚鹹, 1.3300) 更多