Esketamine for Medicinal Chemistry & Drug Development

3 papers and 2 clinical trials exploring esketamine as a treatment for medicinal chemistry & drug development.

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Esketamine

Esketamine (Spravato) is the S-enantiomer of ketamine, approved as an intranasal treatment for treatment-resistant depression and MDD with acute suicidal ideation. It is administered under clinical supervision with post-dose monitoring and has reached over $1.6 billion in annual sales.

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IndicationOver 300 million people worldwide experience depression, with many also suffering from related anxiety disorders.

Medicinal Chemistry & Drug Development

Medicinal chemistry plays a crucial role in the development of novel psychedelic compounds, focusing on their molecular structures and interactions. Researchers utilise innovative methods to enhance safety and efficacy in psychedelic substances.

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Academic Research

3 papers

Open Accessindividual

Efficacy and Safety of Flexibly Dosed Esketamine Nasal Spray Plus a Newly Initiated Oral Antidepressant in Adult Patients with Treatment-Resistant Depression: A Randomized, Double-Blind, Multicenter, Active-Controlled Study Conducted in China and USA

This double-blind, randomised Phase III trial (n=227) finds no significant difference between esketamine plus a new antidepressant versus only the antidepressant (and a placebo) at day 28 on depression scores (MADRS). The study reports one death in the esketamine group. It also states esketamine to be effective and safe though only the first claim could be credibly made if one only looks at the immediate (24-hour) effects.

Published: March 31, 2023
Journal: American Journal of Psychiatry
Authors: Chen, X., Hou, X., Bai, D., Lane, R., Zhang, C., Canuso, C., Wang, G., Fu, D. J.

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Acute effects of ketamine and esketamine on cognition in healthy subjects: A meta-analysis

This meta-analysis assessed the effects of ketamine administration in healthy participants (n=1,041) on several cognitive domains. Deficits in verbal learning/memory were most prominent, whereas response inhibition was the least affected. Negative effects were dependent on infusion dose and plasma level but unaffected by enantiomer type, route of administration, sex or age.

Published: August 1, 2022
Journal: Progress in Neuro-Psychopharmacology and Biological Psychiatry
Authors: Zhornitsky, S., Pelletier, R., Assaf, R., Potvin, S., Li, C-S., Tourjaman, V.

Open Accessindividual

Absence of long-term analgesic effect from a short-term S-ketamine infusion on fibromyalgia pain: A randomized, prospective, double blind, active placebo-controlled trial

In a randomised, double-blind, active placebo-controlled trial of 24 fibromyalgia patients, a 30‑minute S‑ketamine infusion produced transient pain reductions that closely tracked plasma levels but yielded no significant long-term analgesic benefit over an eight‑week follow‑up versus midazolam. Side effects were mild–moderate and declined rapidly, suggesting adequate blinding.

Published: January 13, 2012
Journal: European Journal of Pain
Authors: Noppers, I., Niesters, M., Swartjes, M., Bauer, M., Aarts, L., Geleijnse, N., Mooren, R., Dahanl, A., Sarton, E.

Clinical Trials

2 trials

Not yet recruitingPhase I

KF2024#1-trial: Esketamine Interaction Study

This open-label, Phase I trial (n=12) will investigate the effects of different methods of esketamine administration (28 mg nasal spray vs. 28 mg oral solution) with and without CYP3A4 inhibitors (grapefruit juice or cobicistat) on drug absorption and metabolism.

Started: December 9, 2024
Type: interventional
Blinding: none
Randomized: Yes
Registry ID: NCT06726382

CompletedPhase I

A Phase I Randomized, Placebo Controlled, Double-Blind, Single-Ascending Dose Study of the Safety, Tolerability and Pharmacokinetics of PCN-101 (Arketamine) and a Relative Safety Comparison of PCN-101 and Esketamine in Healthy Volunteers

Phase I, randomized, double-blind, placebo-controlled study in healthy volunteers assessing single ascending IV doses of PCN-101 (arketamine) and a crossover relative safety comparison with esketamine (15 mg IV).

Started: February 25, 2020
Type: interventional
Blinding: double
Randomized: Yes
Registry ID: ACTRN12620000226909

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