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apomorphine (apomorphine, Chiesi / Apofin / Apofin Stylo)

✓ Approved

Chiesi Farmaceutici S.p.A. · DRD2 · 小分子

什么是 apomorphine？

apomorphine 是一种小分子，由Chiesi Farmaceutici S.p.A.研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Subcutaneous Injection。

药物档案

商品名apomorphine, Chiesi, Apofin, Apofin Stylo
公司Chiesi Farmaceutici S.p.A.
药物类别小分子
分子靶点DRD2
给药途径Injectable (Others), Subcutaneous Injection
状态Approved
来源： ClinicalTrials.gov, Chiesi Farmaceutici S.p.A.

作用机制

分子靶点

apomorphine 作用于 1 个分子靶点：

DRD2dopamine receptor D2 (D2DR, D2R)
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

apomorphine 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
Nervous system disordersParkinson's disease✓ Approved

相关研究文献

PubMedFrontiers in immunology2026-09-10

STN-DBS exerts neuroprotection and anti-inflammatory effects in a Parkinson's disease rat model.

Yuan Ying Y, Liu Qidan Q, Liu Peng P, Guo Lili L et al.

Parkinson's disease (PD) is a progressive neurodegeneration disease characterized by dopaminergic (DA) neuron loss, with chronic neuroinflammation. Subthalamic nucleus deep brain stimulation (STN-DBS) is clinically effective for the relief of parkinsonism motor symptoms. Here, we used a homemade device to investigate the effect of STN-DBS on neuroprotection and chronic neuroinflammation in a unilateral 6-hydroxydopamine (6-OHDA)-induced PD rat model. Male Sprague-Dawley rats received 6-OHDA injections into the striatum, followed by ipsilateral STN electrode implantation and high-frequency stimulation. Motor function was assessed by open-field and apomorphine-induced rotation tests. DA neuron survival, glial phenotype changes, and nuclear factor (NF)-κB pathway activity in the nigrostriatal system were evaluated using Western blotting, immunofluorescence, and RT-qPCR. STN-DBS improved motor deficits and decreased the loss of tyrosine hydroxylase-positive neurons. It promoted astrocytes presented a neuroprotective phenotype and increased expression of brain-derived neurotrophic factor, and microglia mainly presented an anti-inflammatory M2 phenotype instead of a pro-inflammatory M1 phenotype. These effects may be associated with IκB-α stabilization, the suppression of NF-κB hyperactivation, and the consequent reduction in the release of downstream pro-inflammatory cytokines. Our findings highlight that our homemade device for STN-DBS is capable of inhibiting NF-κB, modulating glial phenotypes, mitigating neuroinflammation, and ultimately ameliorating parkinsonism deficits.

PMID 42718453
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PubMedJournal of neural transmission (Vienna, Austria : 1996)2026-09-08

Sublingual apomorphine for Parkinsonian tremor: a post-hoc analysis of pivotal trial data.

Dafsari Haidar S HS, Reis João J, Strauß Kerstin K, Brigas Helena C HC et al.

Tremor is a common and disabling feature of Parkinson's disease (PD) and often responds suboptimally to oral dopaminergic therapy. This post‑hoc analysis evaluated tremor outcomes associated with apomorphine sublingual film (SL‑APO) in patients with a tremor‑dominant PD phenotype, using data from a 12‑week randomised, double‑blind, placebo‑controlled trial (NCT02469090) and a 12‑month open‑label study (NCT02542696) conducted in levodopa‑responsive patients with OFF episodes. Tremor‑dominant phenotype was defined according to Movement Disorder Society-Unified Parkinson's Disease Rating Scale (MDS‑UPDRS) criteria, and tremor severity was assessed using a derived tremor index. In the randomised trial, 31 of 108 patients (28.7%) met tremor‑dominant criteria. At Week 12 (n = 10 per group), greater reductions in tremor index scores were observed 30 min post‑dose with SL‑APO versus placebo (mean change - 5.3 vs. - 1.1), with an exploratory between‑group difference of - 4.4 (p < 0.001) and an effect size (Cohen's d) of - 1.83. Clinically important improvement occurred more frequently with SL‑APO (80%) than placebo (30%), corresponding to an estimated number needed to treat of 1.3. Median time to ON with SL‑APO was 13.0 min. In the open‑label study, tremor reductions of 31-37% were maintained over 12 months, with responder rates remaining above 70%. These exploratory findings in a small subgroup are consistent with a potential for early and maintained tremor improvement with SL‑APO in patients with tremor‑dominant PD; however, the results are hypothesis‑generating and require prospective confirmation.

PMID 42709169
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PubMedSchizophrenia research2026-09-07

Ovariectomy reverses maternal immune activation-induced deficits in dopamine and NMDA receptor-mediated regulation of prepulse inhibition in female Long-Evans rats.

van den Buuse Maarten M, Sbisa Alyssa A, Gogos Andrea A

We studied the role of ovarian steroid hormones in the poly(I:C) maternal immune activation model of schizophrenia in rats. Pregnant Long-Evans rats were injected IV with 4 mg/kg of poly(I:C) on gestational day 15. In adult female offspring, we measured prepulse inhibition (PPI) and its disruption by acute treatment with the dopamine receptor agonist, apomorphine (APO), and the NMDA receptor antagonist, MK-801, and compared intact controls and intact poly(I:C) offspring with ovariectomised (OVX) controls and OVX poly(I:C) offspring. PPI was significantly reduced at baseline in intact poly(I:C) rats and the disruption of PPI caused by APO and MK-801 was diminished. Similar effects were observed following OVX in control rats. In contrast, following OVX in poly(I:C) rats, baseline PPI was similar to that found in intact controls and APO and MK-801 significantly reduced PPI in these animals. These results show that OVX reverses the effects of maternal immune activation on PPI and its regulation by dopamine and NMDA receptors. It is likely that the effect of maternal immune activation on PPI regulation involves a delicate endocrine imbalance, most likely involving altered ovarian steroid hormones levels, the effect of which may be reversed by OVX. These results expand our insight into the possible mechanism of action of novel steroid hormone compounds currently trialled for schizophrenia.

PMID 42704947
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PubMedRevue neurologique2026-09-03

Effect of levodopa-carbidopa intestinal gel infusion on objective measures of daytime sleepiness and nocturnal sleep in Parkinson's disease.

Bucy M M, Carpentier N N, Clement G G, Richard S S et al.

Excessive daytime sleepiness and sleep disturbances are common in Parkinson's disease (PD), considerably affecting the quality of life of patients and caregivers. Antiparkinsonian medications further complicate sleep-wake management. Advanced PD with motor fluctuations often requires continuous dopaminergic stimulation via apomorphine subcutaneous infusion or levodopa/carbidopa intestinal gel infusion (LCIGI). Evidence on LCIGI's effects on sleep and sleepiness remains limited, relying mainly on subjective bias-prone measures. This pilot study used overnight in-laboratory polysomnography (PSG) and the multiple sleep latency test (MSLT), the gold standards for objective measurements, to evaluate effects of LCIGI initiation on sleep and sleepiness. In this prospective, monocentric observational study, 34 patients with motor fluctuations underwent PSG and MSLT before (M0) and three months after (M3) LCIGI initiation. Clinical characteristics included body mass index (BMI), L-Dopa equivalent daily dose (LEDD), and Epworth Sleepiness Scale (ESS) scores to examine correlations between subjective questionnaire-based and objective MSLT-based measures. Twenty-three patients completed both assessments. MSLT values remained stable (M0: 12.5 [10.9; 15.8] min; M3: 15.3 [12.2; 16.6] min; P=0.401) as did PSG parameters. As expected, BMI decreased, LEDD increased, dopamine agonist use declined, and clozapine/quetiapine use increased. ESS scores did not correlate with MSLT results at baseline or follow-up. LCIGI had no significant impact on objectively measured daytime sleepiness (MSLT) or PSG sleep parameters.

PMID 42692964
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PubMedZhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica2026-09-03

[Effects of Compound Dihuang Granules on PERK/ATF4/CHOP pathway in substantia nigra of rat model of Parkinson's disease with syndrome of Yin deficiency and stirring wind].

Ma Xin X, Liang Jian-Qing JQ, Wan Ying-Qin YQ, Zhang Zhen-Chang ZC et al.

This study aims to investigate the therapeutic mechanism of Compound Dihuang Granules in a rat model of Parkinson's disease(PD) with the syndrome of Yin deficiency and stirring wind, by examining their effects on the expression of activating transcription factor 4(ATF4), CCAAT/enhancer-binding protein homologous protein(CHOP), eukaryotic initiation factor 2 alpha(eIF2α), and protein kinase RNA-like endoplasmic reticulum kinase(PERK) in the substantia nigra. A rat model of PD with the syndrome of Yin deficiency and stirring wind was established via unilateral injection of 6-hydroxydopamine into the substantia nigra. Seventy-five successfully modeled rats were randomly assigned to a model group, a madopar group, and low-, medium-, and high-dose Compound Dihuang Granules groups, each receiving the corresponding agents by oral gavage. Additional 30 rats were allocated to a normal control group and a sham-operated group. The two groups, together with the model group, were administered an equal volume of normal saline. Behavioral performance was evaluated by the apomorphine-induced rotation test, pole-climbing test, and hanging test. Histopathological alterations and ultrastructural changes in the substantia nigra were assessed by HE staining and transmission electron microscopy. Furthermore, immunohistochemistry, Western blot, and RT-qPCR were employed to quantify the protein and mRNA levels of ATF4, CHOP, eIF2α, phosphorylated(p)-eIF2α, PERK, and p-PERK in the substantia nigra tissue. Compared with the normal control and sham-operated groups, the model group exhibited a reduction in hanging time(P<0.01), accompanied by increases in rotation count and pole-climbing time(P<0.01). Compared with the model group, the madopar group and all Compound Dihuang Granules groups demonstrated improvements in behavioral performance, as evidenced by prolonged hanging time(P<0.05), reduced rotation count(P<0.01), and shortened pole-climbing time(P<0.01). These functional improvements were paralleled by attenuation of neuronal injury in the substantia nigra and amelioration of mitochondrial ultrastructural abnormalities. Western blot and RT-qPCR analyses revealed that Compound Dihuang Granules dose-dependently downregulated the protein and mRNA levels of key molecules in the PERK/ATF4/CHOP signaling pathway(P<0.05 or P<0.01). Notably, the effects observed in the high-dose group were comparable to those of the madopar group. Compound Dihuang Granules may exert neuroprotective effects in the rat model of PD with the syndrome of Yin deficiency and stirring wind by suppressing the PERK/ATF4/CHOP signaling pathway, thereby alleviating endoplasmic reticulum stress and neuronal apoptosis. These findings provide experimental support for the clinical study of Compound Dihuang Granules in the treatment of PD.

PMID 42693021
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PubMedGeneral hospital psychiatry2026-09-01

Neurostimulants for disorders of consciousness in the intensive care unit: A systematic review.

Gunther Matthew M, Tran Nathan N, Prothro Katherine K, Huddleston Boglarka B et al.

Disorders of consciousness (DoC; encompassing coma, unresponsive wakefulness syndrome, and minimally conscious state) are sequelae of critical illness that prolong hospitalization and interfere with engagement in care. Due to heterogeneous and incompletely understood pathophysiology, no pharmacologic standard of care has been established. We aimed to systematically examine the efficacy, safety, and dosing of neurostimulants among adult ICU patients with DoC. We conducted a systematic search of PubMed, Embase, CINAHL, and Web of Science from inception to December 2025. Studies that examined the use of neurostimulants for DoC in critically ill adults were included. We followed Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines and used the Effective Public Health Practice Project framework to appraise bias. 35 studies met inclusion criteria: 11 randomized controlled trials, 19 observational, and 5 case-based studies. Amantadine was the most studied agent (N = 2743), with several studies reporting improvements in standardized measures of consciousness and earlier transition to rehabilitation. Modafinil (N = 1776) was primarily evaluated for hypersomnolence and demonstrated mixed effects on Glasgow Coma Scale (GCS) scores. Methylphenidate (N = 1044) demonstrated signals of benefit in both randomized studies and augmentation strategies with amantadine. Apomorphine was evaluated in one placebo-controlled ICU trial and carbidopa-levodopa in one case series. Despite inclusion in our search strategy, no studies examined caffeine, amphetamines, or bromocriptine. Neurostimulants were associated with short-term improvements in measures of arousal and recovery, although evidence remains heterogeneous and largely observational. Amantadine has the largest ICU evidence base; methylphenidate has been studied as monotherapy and augmentation; modafinil has primarily been evaluated for hypersomnolence. Further placebo-controlled trials are needed to establish efficacy across different causes of DoC; head-to-head studies are needed to clarify comparative effectiveness among available neurostimulants.

PMID 42679710
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