Introduction to Biopharmaceuticals

UG Course

Touqeer Ahmed Ph.D. Atta-ur-Rahman School of Applied Bioscience

National University of Sciences and Technology 9th September, 2014

Course ContentsBiopharmaceuticals• Introduction to the Biopharmaceuticals/drugs• Pharmacokinetic and Pharmacodynamics• Introduction to biopharmaceuticals and their

Pharmacokinetics • Active Pharmaceutical Ingredient (API) and

Drug Product Specifications• Biopharmaceutical Products:

– Antibodies• Monolconal • Polyclonal• Bi-specific

– Hormones– Enzymes – Interferon– Thrombolytic agents (tissue plasminogen

activator)• Drug Development and its phases

Kinetics of Biopharmaceuticals

•One Compartment Open Model ' IV Bolus Injection

•Multicompartmental Models ' IV Bolus Injection

•Drug Elimination and Clearance

•Pharmacokinetics of Oral Absorption

•Multiple Dosage Regimens

•Nonlinear Pharmacokinetics

•Physiologic Drug Distribution and Protein Binding

•Renal and Hepatic Elimination of Drugs

•Bioavailability and Bioequivalence

•Immunogenicity of Biopharmaceuticals

•Regulatory Compliance for Biopharmaceuticals and

Biologics

•Application of Pharmacokinetics in Clinical Situations

Recommended Books

• Assignments 10• Quiz 20• First Sessional 10• Second Sessional 10• Final Exams (Terminal Exams) 50

Evaluation System

Introduction to Biopharmaceuticals/Drugs

Touqeer Ahmed Ph.D. Atta-ur-Rahman School of Applied Bioscience,

National University of Sciences and Technology,Islamabad

17th September, 2014

DrugsIn the most general sense, a drug may be defined as any substance that bringsabout a change in biological function through its chemical actions.

• Drugs may be – Hormones synthesized in the body– Xenobiotics not synthesized in the body – Poisons drugs having exclusively harmful effect (e.g. lead and arsenic)– Toxins are usually defined as poisons of biologic origin syntehsized by the plants and

animals)

1. PHYSICAL NATURE– solid at room temperature (eg, aspirin, atropine), – liquid (eg, nicotine, ethanol) – gas (eg, nitrous oxide).

2. DRUG SIZE ((lithium ion, MW 7) to very large (eg, alteplase [t-PA], a protein of MW 59,050)

3. DRUG SHAPE (Chirality (stereoisomerism)4. DRUG REACTIVITY AND DRUG-RECEPTOR BONDSCovalent, electrostatic and hydrophobic

Drug and Medicine

• What is a drug?– A drug can be defined as a chemical substance of known (and sometimes unknown

structure), other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect.

– To count as a drug, the substance must be administered, rather than released by physiological mechanisms. Many substances, such as insulin or thyroxine, are endogenous hormones but are also drugs when they are administered intentionally.

• What is a medicine?– A medicine is a chemical preparation, which usually but not necessarily contains one

or more drugs, administered with the intention of producing a therapeutic (healing/recovery from disease) effect.

– Medicines usually contain other substances (excipients, stabilisers, solvents, etc.) besides the active drug, to make them more convenient to use.

Biopharmaceuticals

• Biopharmaceuticals are the drugs which are produced using biotechnology. They include proteins (including antibodies), nucleic acids and living microorganisms like virus and bacteria where their virulence is reduced by the process of attenuation.

Biopharmaceuticals

Biopharmaceutics

• The study of the chemical and physical properties of drugs, their components, and their activities in living organisms.

Drug release and dissolutions

Drug in systemic circulation

Excretion and metabolism

Pharmacological effect

Drug in tissues

Biopharmaceutics

Pharmacokinetics and Pharmacodynamics

• Pharmacokinetics deals with the study of kinetics of drug absorption, distribution and elimination

• Elimination: is composed of collective processes of excretion and metabolism• Drug disposition: collectively drug distribution and elimination

Clinical pharmacokineticsStudy of the drug kinetics based on the clinical observations such as the patients disease state and patient specific consideration (e.g. age, sex and ethnicity)

PharmacodynamicsDeals with the study of drug concentration at the site of action and the pharmacologic response produced by the drug.

• Protein targets for drug binding Four main kinds of regulatory protein are commonly involved as primary

drug targets, namely: 1.receptors (activate signaling pathways) 3.enzymes 2. carrier molecules (transporters) 4.ion channels.

Drug Targets

• Agonists and antagonists

Agonists, which 'activate' the receptors, and antagonists, which combine at the same site and block the effect of agonists by inhibiting the activation ofreceptors.