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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

PubMedThe Journal of neuroscience nursing : journal of the American Association of Neuroscience Nurses2026-08-03

Initiating Apomorphine Therapy Without Antiemetic Pretreatment: Real-World Data From a Nurse-led Parkinson Disease Support Program.

Happel Cindy C, Grall Mindy M, Formella Andrea A

Trimethobenzamide has been the antiemetic of choice in the United States for people with Parkinson disease initiating subcutaneous apomorphine injection (SC-APO) therapy to rapidly manage OFF episodes. Following a cessation of trimethobenzamide production in 2021, SC‑APO was increasingly initiated without antiemetic pretreatment. Data from the SC-APO Clinical Nurse Navigator support program were analyzed for new patient starts between January 2019 and March 2024, spanning periods before and after trimethobenzamide absence and SC-APO labeling changes. SC-APO starting dose patterns and 90-day treatment continuation were compared between patients who started with and without antiemetic pretreatment. Among 2634 patients, SC-APO initiations without trimethobenzamide increased from 32.8% before cessation of production (2019-2020) to nearly 100% by the end of 2021. During 2021, most prescribers (56.7%) continued to use the 0.2 mL (2.0 mg) starting dose; following a 2022 labeling update, use of the 0.1 mL (1.0 mg) starting dose increased to 86% by early 2024. The 90-day SC-APO continuation rates increased from 75.4% when used with trimethobenzamide pretreatment to 83.1% without it. SC-APO is now routinely started without antiemetic pretreatment, with higher overall rates of early treatment continuation. Flexible starting doses and titration, together with nurse‑led patient education and support, may facilitate successful treatment initiation and continuation in contemporary clinical practice.

PMID 42545868
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PubMedIBRO neuroscience reports2026-08-02

Reduced DJ-1/Nrf2/HO-1 antioxidant signalling is associated with type 2 diabetes-related aggravation of neurodegeneration in a mouse model of Parkinson's disease.

Xu Honghao H, Li Mengjia M, Li Yujia Y, Zou Zhuochi Z et al.

Parkinson's disease (PD) and type 2 diabetes mellitus (T2DM) are increasingly recognized as comorbid conditions. Epidemiological evidence suggests that T2DM is associated with faster PD progression, but the biological processes that may connect these disorders remain incompletely understood. Oxidative stress is a shared pathological feature of both diseases, and the DJ-1/Nrf2/HO-1 pathway is an important antioxidant defence system. To determine whether T2DM is associated with more severe PD-like neurodegeneration and whether these changes are accompanied by reduced DJ-1/Nrf2/HO-1 antioxidant signalling in a mouse model of PD-T2DM comorbidity. Male C57BL/6 mice were assigned to control, T2DM, PD, or PD + T2DM groups. T2DM was induced by high-fat diet feeding combined with streptozotocin injection; PD was induced by unilateral intrastriatal 6-hydroxydopamine injection. Behavioural performance was assessed using rotarod and apomorphine-induced rotation tests. Nigrostriatal pathology was examined by haematoxylin-eosin, Nissl, and tyrosine hydroxylase immunohistochemistry. Oxidative stress markers (SOD, MDA, GSH) and DJ-1/Nrf2/HO-1 protein expression were measured in substantia nigra-striatum and serum. Final analyses included 10 control, 9 T2DM, 9 PD, and 9 PD + T2DM mice, with assay-specific sample sizes indicated in the Methods and figure legends. Compared with PD mice, PD + T2DM mice exhibited shorter rotarod latency, greater dopaminergic neuron loss, and stronger nigrostriatal oxidative stress (P < 0.05). DJ-1, Nrf2, and HO-1 expression was reduced in the substantia nigra-striatum of disease groups relative to controls, with Nrf2 and HO-1 significantly lower in PD + T2DM than in PD mice. Protein expression correlated positively with rotarod latency and antioxidant indices, and negatively with MDA content and fasting glucose. Serum oxidative stress markers showed similar directional trends, but most between-group differences were not statistically significant. In this combined toxin- and metabolism-based mouse model, T2DM was associated with more severe PD-like motor impairment and dopaminergic neuron loss, accompanied by reduced DJ-1/Nrf2/HO-1 antioxidant signalling and increased nigrostriatal oxidative stress. These findings are consistent with the possibility that impaired antioxidant defence contributes to PD-T2DM comorbidity, while causal pathway involvement requires confirmation by future gain- or loss-of-function studies.

PMID 42542636
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PubMedAdvanced pharmaceutical bulletin2026-07-29

Clinical Studies Using Intranasal Therapies for Parkinson's Disease: A Review.

Vahidi Ramin R, Bukanian Mahsa M, Kachooeian Maryam M

Intranasal delivery is a method of administering medications through the nasal cavity. It offers several advantages, such as rapid absorption, bypassing first-pass metabolism, direct nose-to-brain transport and localized effects. These benefits make it a promising approach for drug delivery in Parkinson's disease, a progressive neurological disorder characterized by the degeneration of nerve cells in the brain. This review evaluates the efficacy and safety of intranasal delivery for Parkinson's disease treatment. Several studies on intranasal apomorphine reported rapid clinical response, improved UPDRS motor scores, tapping scores, and median Webster's scores, suggesting its effectiveness as a rescue therapy during "off" states. Intranasal recombinant erythropoietin was well tolerated and showed cognitive benefits. intranasal glutathione was safe and showed better bioavailability. Intranasal insulin improved cognitive performance without hypoglycemia, indicating a localized effect. Intranasal cholecystokinin and ipratropium bromide did not show significant benefits. Intranasal desmopressin is a safe and effective medication for nocturnal polyuria in Parkinson disease. Intranasal transplantation of neural stem cells is safe and is associated with functional improvement. Finally, Rivastigmine nasal spray offered better bioavailability and fewer side effects compared with conventional forms. The most common adverse effect was mild transient nasal or throat irritation. This review highlights the potential applications, efficacy, and side effects of various intranasal medications for Parkinson's disease and proposes using new interventions for future studies. The general benefits of nasal administration for Parkinson's disease treatment include localized effects, fewer side effects, faster onset of action, improved bioavailability, and enhanced therapeutic effectiveness.

PMID 42524014
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PubMedBrain sciences2026-07-28

Effects of Continuous Infusion Therapies on Non-Motor Symptoms in Advanced Parkinson's Disease: A Systematic Review.

Rinaldi Domiziana D, De Carolis Lanfranco L, Ledda Claudia C, Galli Silvia S et al.

Background/Objectives: Non-motor symptoms (NMS) are highly prevalent in advanced Parkinson's disease (PD) and substantially affect quality of life. Continuous infusion therapies are established treatment options for motor fluctuations not controlled by oral medication, but their effects on NMS remain incompletely characterized. We aimed to evaluate the effects of continuous infusion therapies on NMS in advanced PD. Methods: A systematic review was conducted according to PRISMA guidelines. PubMed, Embase, and Cochrane were searched for English-language original studies published between January 2005 and 1 March 2026. Eligible studies included patients with PD treated with levodopa-carbidopa intestinal gel (LCIG), continuous subcutaneous apomorphine infusion (CSAI), subcutaneous levodopa formulations, or levodopa-entacapone-carbidopa intestinal gel (LECIG) and reported quantitative NMS outcomes. Due to methodological heterogeneity, results were synthesized qualitatively. Results: Fifty-four studies were included. Most evaluated LCIG (n = 38), followed by CSAI (n = 14), subcutaneous levodopa formulations (n = 6), and LECIG (n = 2). Overall, 4157 patients were assessed at baseline and 2919 at follow-up. Global non-motor burden improved in 33/45 (73.3%) baseline-to-follow-up comparisons. NMSS total score decreased from 84.4 ± 35.2 to 54.9 ± 17.6. The most consistent benefits were observed for sleep/fatigue and gastrointestinal symptoms. Sleep/fatigue outcomes improved in 26/31 (83.9%) baseline-to-follow-up comparisons. Cognitive outcomes were mostly stable, while cardiovascular, urinary, sexual, and mood-specific outcomes showed less consistent benefit. Conclusions: Continuous infusion therapies may be associated with reduced global non-motor burden in advanced PD, particularly sleep/fatigue and gastrointestinal symptoms. Evidence is strongest for LCIG, while data for CSAI, LECIG, and subcutaneous levodopa formulations remain limited.

PMID 42512473
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PubMedPharmacoEconomics2026-07-15

Inhaled Levodopa for the Management of OFF Episodes in Parkinson's Disease: A Cost-Effectiveness Analysis.

Evans Daniel D, Mistry Chetan C, Knight Harun H, Shah Rushab R et al.

OFF episodes in Parkinson's disease (PD), where symptoms worsen despite symptomatic treatment, are associated with significant burden on patients, carers and healthcare providers. There is an unmet need for an effective, on-demand treatment for OFF episodes that provides fast-acting symptom relief. This study estimated the cost-effectiveness of inhaled levodopa (LD) compared with relevant alternatives from a UK National Health Service and Personal Social Services perspective. A Markov model was developed comparing inhaled LD with subcutaneous (SC) apomorphine, sublingual (SL) apomorphine, dispersible LD and no on-demand treatment (no-ODT) in adults with advanced PD treated with LD and carbidopa and experiencing OFF episodes. A lifetime time horizon was adopted. Within-trial and beyond-trial models were applied for initial treatment and subsequent therapy, respectively. Model structure comprised 12 health states: ten 'Off' states, an 'On' state and death. Clinical trials and a network meta-analysis informed clinical inputs, with natural history progression applied from year 3. UK national databases and published literature informed costs (2025) and utility data. A 3.5% yearly discount rate is applied to costs and outcomes. Sensitivity analyses and three scenarios exploring alternative progression through health states, caregiver costs and disutilities, as well as subsequent therapy adverse events, were conducted. In base-case analysis, inhaled LD dominated versus dispersible LD and no-ODT and was associated with lower cost and lower quality-adjusted life years (QALYs) versus SC and SL apomorphine. Nevertheless, inhaled LD resulted in net monetary benefit (NMB) of £14,226 and £25,939 compared with SC and SL apomorphine, respectively, at a £25,000 willingness-to-pay threshold. Key model drivers were subsequent therapy costs, discontinuation rates and health state utility values. The probabilistic sensitivity analysis highlighted uncertainty in the model; however, mean probabilistic sensitivity analysis results, along with two scenario analyses, remained consistent with the base case. Inhaled LD may be an economically dominant treatment strategy when compared with dispersible LD and no-ODT. When compared with SC and SL apomorphine, cost-savings with inhaled LD may outweigh potentially fewer QALYs, resulting in an NMB.

PMID 42455231
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PubMedNeurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology2026-07-15

Device aided therapies in Parkinson disease: an expert view on apomorphine.

Stocchi Fabrizio F, Ceravolo Roberto R, Colosimo Carlo C, De Pandis Maria Francesca MF et al.

Parkinson's disease (PD) affects approximately 1% of individuals over the age of 60, with its prevalence increasing in older populations. Clinical manifestations can be effectively controlled during the first years of disease but progressively medications effect shortens with appearance of motor complications and dyskinesia. Management of PD primarily aims to restore dopaminergic activity through pharmacological interventions such as levodopa, which effectively alleviates motor symptoms and extends life expectancy. Early initiation of treatment improves bradykinesia, rigidity, and tremor; however, as the disease advances, the therapeutic response to levodopa shortens, leading to complications such as motor fluctuations and dyskinesia. In advanced Parkinson's disease (aPD), the emergence of the "wearing-off" phenomenon and unpredictable "on/off" fluctuations-where symptoms reappear despite medications-poses significant challenges for disease management. Device-aided therapies, including deep brain stimulation and continuous infusion of apomorphine or levodopa, provide effective management options for advanced Parkinson's disease (aPD) when oral medications fail to adequately control symptoms. Continuous subcutaneous apomorphine infusion (CSAI) has demonstrated both efficacy and long-term tolerability; however, its clinical adoption remains limited due to challenges in patient selection and referral, treatment initiation and handling of the device. This review examines the available infusion therapies, with a particular focus on CSAI, and aims to provide clinicians with evidence-based guidance for optimizing treatment selection in aPD.

PMID 42455202
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