Iprindole   中文名称: 伊普吲哚

伊普林多具有抗抑郁活性，并且是去甲肾上腺素和5-羟色胺摄取的弱抑制剂。
伊普林多是一种三环类抗抑郁药（TCA），与传统TCA相比，其药理学特性有所不同。它的分子式为C19H28N2，分子量为284.44。它的作用和用途与阿米替林相似，但抗胆碱能和镇静作用较弱。伊普林多的ATC代码为N06AA13。研究表明，与传统TCA相比，伊普林多具有抗抑郁疗效，且镇静和心血管副作用更少。

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# Iprindole (Prondol, indole-type atypical tricyclic antidepressant, Wyeth, fully global withdrawn due idiosyncratic hepatotoxicity)
Single oral ascending dose first-in-human Phase 1 safety, tolerability, CNS PK and monoamine PD biomarker study of oral Iprindole in healthy adult volunteers
CTID: Not Applicable
Phase: Phase 1 SAD
Status: Completed
Date: 1964

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Phase 1 multiple daily oral dosing crossover PK substudy evaluating food effect, age and mild hepatic/renal impairment on systemic plasma Iprindole exposure and circulating metabolites
CTID: Not Applicable
Phase: Phase 1 MAD PK Substudy
Status: Completed
Date: 1965

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Phase 1 neurophysiology PD substudy measuring sleep architecture (unique non-REM-suppressing profile) and central 5-HT2/H1 receptor target engagement via polysomnography
CTID: Not Applicable
Phase: Phase 1 CNS Imaging/Sleep PD Substudy
Status: Completed
Date: 1965

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Randomized double-blind placebo-controlled Phase 2 dose-ranging trial of oral Iprindole for mild-to-moderate outpatient major depressive disorder; primary endpoint HAMD total score change at week 4
CTID: Not Applicable
Phase: Phase 2 Dose-Ranging
Status: Completed, positive efficacy signal
Date: 1966

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Multicenter double-blind active-controlled Phase 3 comparative trial: Iprindole vs Imipramine for moderate depression, comparing antidepressant potency, anticholinergic sedative adverse event burden
CTID: Not Applicable
Phase: Phase 3 Head-to-Head Comparative
Status: Completed
Date: 1974

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Open-label long-term Phase 3 extension safety maintenance study (12-month chronic dosing) monitoring liver function enzymes, jaundice, rash and eosinophilia adverse signals
CTID: Not Applicable
Phase: Phase 3 Long-Term Safety Extension
Status: Terminated early post emerging hepatic injury cases
Date: 1978

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Post-marketing Phase 4 multinational pharmacovigilance observational registry documenting idiosyncratic cholestatic jaundice risk leading to progressive market restriction and full withdrawal
CTID: Not Applicable
Phase: Phase 4 Post-Marketing Safety Surveillance
Status: Completed
Date: 1982

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Retrospective pooled Phase 2/3/Phase4 safety subanalysis stratifying hepatotoxicity incidence by treatment duration, age and concurrent medication exposure
CTID: Not Applicable
Phase: Retrospective Safety Substudy
Status: Completed
Date: 1983

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Discontinued exploratory Phase 2 proof-of-concept trial planned for generalized anxiety disorder (halted after hepatic safety risk confirmed)
CTID: Not Applicable
Phase: Planned Phase 2 PoC Anxiety
Status: Discontinued
Date: 1984

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Preclinical in vitro radioligand receptor binding assay profiling Iprindole pharmacology: potent 5-HT2A/2C & H1 antagonist, weak SERT/NET reuptake inhibition, low muscarinic/α-adrenoceptor affinity vs classic TCAs
CTID: Not Applicable
Phase: Preclinical Biochemical Receptor Profiling
Status: Completed
Date: 1962

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Ex vivo rodent brain slice electrophysiology preclinical study measuring 5-HT-mediated synaptic transmission modulation without profound monoamine transporter blockade
CTID: Not Applicable
Phase: Preclinical Neurophysiology
Status: Completed
Date: 1963

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In vivo rodent behavioral efficacy preclinical trial: reversal of reserpine-induced behavioral despair, antidepressant activity with minimal REM sleep suppression phenotype
CTID: Not Applicable
Phase: Preclinical CNS Behavioral Efficacy
Status: Completed
Date: 1963

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28-day & 90-day repeat oral dose general toxicology preclinical trial of Iprindole in rats and beagle dogs; preclinical liver signals mild, failed to predict human idiosyncratic cholestatic hepatotoxic liability
CTID: Not Applicable
Phase: Preclinical Chronic Toxicology
Status: Completed
Date: 1964

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Radiolabeled [³H]-Iprindole whole-body ADME biodistribution preclinical study confirming moderate blood-brain barrier penetration and hepatic phase II glucuronidation primary clearance pathway
CTID: Not Applicable
Phase: Preclinical ADME Metabolism
Status: Completed
Date: 1965

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Modern comparative mechanistic preclinical follow-up research using Iprindole as chemical probe to dissect 5-HT2 receptor-mediated mood regulation pathways and atypical antidepressant scaffold SAR
CTID: Not Applicable
Phase: Preclinical Mechanism Follow-Up Research
Status: Completed
Date: 2023