Selective Serotonin Reuptake Inhibitors – Challenges for Drug Discovery

These flashcards cover key concepts related to selective serotonin reuptake inhibitors and challenges in drug discovery, based on lecture notes.

What is an SSRI?

A Selective Serotonin Reuptake Inhibitor, a class of drugs used to treat depression by increasing serotonin levels in the brain.

What are the major phases in the drug discovery process?

Target Identification, Hit Identification, Hit-to-Lead, Lead Optimisation, Preclinical Development, Clinical Trials (Phases I to III), and Marketing Authorisation.

What challenge does drug discovery face for CNS drugs?

The difficulty of getting drugs across the blood-brain barrier and understanding their actions on complex human conditions.

How much can drug discovery cost?

The cost can range from $1 billion to $12 billion.

What was significant about the discovery of sertraline?

Sertraline, discovered in the 1970s, is based on structures of known neuroleptic compounds and acts as an SSRI.

What were the results of the animal tests for SSRIs?

The animal tests had weak links to human conditions and mainly established toxicity and safety.

What is the role of the FDA in drug approval?

The FDA requires pharmacological and toxicological information before approving a drug for clinical investigations.

What are some alternative funding models for drug discovery?

Funds from organizations like the Bill and Melinda Gates foundation, Cancer Research UK, or the NHS budget.

How did the patent status affect Zoloft?

Zoloft generated $3.3 billion in sales for Pfizer before its patent expired in June 2006.

What is the importance of data publication in drug discovery?

Publishing all data, including negative results, allows for better decision-making regarding drug efficacy.

What is the blood-brain barrier?

The blood-brain barrier is a selective permeability barrier that separates the circulating blood from the brain and extracellular fluid in the central nervous system.

What are neuroleptic compounds?

Neuroleptic compounds are medications used to manage psychosis, particularly in schizophrenia, and their structures served as a basis for developing SSRIs like sertraline.

What is clinical trial Phase I?

Phase I clinical trials primarily focus on determining a drug's safety, dosage, and side effects in a small group of healthy volunteers.

What is clinical trial Phase II?

Phase II clinical trials assess the effectiveness of a drug on a particular disease or condition, involving a larger group of patients.

What are clinical trial Phase III tests?

Phase III clinical trials compare the new drug to standard treatments in large populations to evaluate effectiveness and monitor side effects.