In this blog post I will demonstrate the development of a new medicine, The name is Evertzolam. A newly AI designed benzodizepine drug that is molecularly designed not to be addicive like other benzodizepine drugs. The idea origins from myself. From 2018 to 2022 I have been addicted to Diazepam. A drug from the Benzodizepine family. It was bad and gave me bad seizures and spasms during my withdrawal period. The drawbacks of the medication far outweighed its benefits. Diazepam is a good and useful medicine. The drawbacks of the however far outweigh its benefits.
In this blog post the newly designed pharmaceutical was designed using OpenAI Chatgpt 4o. It could also have been done with equal models. (DeepSeek R1 for example.The prompt used was “design a new drug called evertzolam. A non addictive benzodizepine drug”.
The reason why it works is because modern LLM’s have been trained on basic Organic Chemistry and know enough about the chemistry and biology to be able to make predictions about how small changes in structure of the organic molecule will change it’s biological effects on people. This includes the addictive properties of substances.
Evertzolam is a novel benzodiazepine analogue designed to provide anxiolytic, sedative, muscle relaxant, and anticonvulsant effects while minimizing the risks of addiction, tolerance, and dependence associated with traditional benzodiazepines like alprazolam, diazepam, and lorazepam.
Structure
AI in this example made a few structural changes to the molecule of Diazepam and created the theoretical Evertzolam which has far less addictive properties but keeps most of the useful effects of Diazepam.
Because AI has designed the molecule, it knows all of it’s chemical properties and structure. With this information, the researchers can synthesize small amounts of Evertzolam and administer it in the expected effective dosage to volunteers of a clinical study.
How to proof that it will work as expected?
Simple. By trying it out on humans. In the world of pharmology the process of trying out (new) medicines is called Clinical studies or Clinical Trials.
This works as follows:
Usually volunteers who joined the study. Are dvided into 2 groups. One receive the actual Evertzolam and the other receive a non active substance or placebo (like sugar). Both groups are then monitored during an extended period of time. The members of both groups don’t know if they were administered the real substance (Evertzolam) or the Placebo. Also nobody involved (doctors and researchers) in the clinical study knows exactly who got what. We scientists say that the study is carried out double blind This is called double blind. It appears to be very essential for these types of studies.
Study outcomes need to be replicable (eg: can be replicated by others without changing the outcome). It has been observed that this works better when the study has been conducted double blind
Overview.
Molecular Structure & Pharmacodynamics
Class: Modified Benzodiazepine
Core Structure: Benzodiazepine scaffold with a substituted GABA_A receptor modulator
Binding Affinity: Selectively targets α2 and α3 subunits of GABA_A receptors while sparing α1 and α5, which are linked to addiction and cognitive impairment.
Mechanism of Action:
Enhances GABAergic neurotransmission without full agonist activity at α1 subunits, reducing euphoria and addiction potential.
Partial allosteric modulation, providing anxiolytic and muscle relaxant effects while avoiding sedative overdose risks.
Slow dissociation rate to prevent withdrawal symptoms.
Key Properties
Non-Addictive Mechanisms
1. Selective α2/α3 Modulation – Targets anxiolytic and muscle-relaxant effects without acting on α1 (which induces euphoria and sedation).
2. Partial Agonism – Reduces dopaminergic reinforcement in the ventral tegmental area (VTA), unlike classical benzodiazepines.
3. Extended-Release Formulation – Prevents spikes in plasma levels, reducing the risk of craving and misuse.
4. GABA_A Receptor Desensitization Avoidance – Unlike diazepam, which leads to receptor downregulation, Evertzolam has built-in receptor recycling properties, preventing rapid tolerance.
5. NMDA Modulation – Includes an NMDA receptor stabilizer to reduce withdrawal symptoms.
Indications
Generalized Anxiety Disorder (GAD)
Panic Disorder
Insomnia (Short-term use)
Muscle Spasms
Epilepsy (Adjunctive therapy)
Potential Side Effects
Mild drowsiness (first few doses)
Dizziness
GI discomfort
No significant cognitive impairment
Conclusion
Evertzolam represents a new generation of benzodiazepines with a high safety margin, minimal addiction risk, and sustained anxiolytic effects. By selectively targeting GABA_A subunits and incorporating novel partial agonist properties, it eliminates tolerance, dependence, and abuse potential—making it a groundbreaking option in the treatment of anxiety, panic disorders, and muscle spasms.
Will it work? Yes, it will probably work like expected.
What are the costs? Since Evertzolam has never been on the market before, this medicine has to undergo all the tests and research that has been put in the original Diazepam. Wich was expensive. The research has to answer all questions about the substance like:
Acute Toxicity: Determines the immediate effects of a single or short-term exposure to the drug.
Chronic Toxicity: Assesses long-term effects of repeated exposure over extended periods.
Genotoxicity: Evaluates whether the drug can cause genetic mutations or DNA damage.
Carcinogenicity: Studies whether the drug has the potential to cause cancer.
Reproductive and Developmental Toxicology: Examines the drug’s impact on fertility, pregnancy, and fetal development.
2. Safety
Preclinical Safety Studies: Conducted in vitro (lab-based) and in vivo (animal studies) to determine potential risks.
Clinical Safety Studies (Phases I–III): Monitor adverse effects, dose-response relationships, and interactions with other drugs.
Post-Market Surveillance (Phase IV): Long-term monitoring of safety in a broader population.
3. Security (Regulatory Compliance & Quality Control)
Good Manufacturing Practices (GMP): Ensures the drug is consistently produced and controlled according to quality standards.
Regulatory Approval: Compliance with agencies like EMA (Europe), FDA (USA), and WHO for approval before commercialization.
Pharmacovigilance: Continuous monitoring of drug effects after approval to detect any previously unknown risks.
4. Safety vs. Efficacy Balance
Therapeutic Index (TI): Compares the effective dose (ED50) to the toxic dose (TD50) to determine the margin of safety.
Benefit-Risk Assessment: Determines whether the benefits of the drug outweigh its risks.
All has to be reached again from scratch. Costing about 4 to 5 billion us dollar. Making it less attractive for the pharmaceutical companies to invest in.
Who is the inventor of Evertzolam?
I am the inventor because I first described it here. I don’t know if it’s going to make me rich or famous yet. Of course I hope so.
