Polypharmacology, 1st ed. 2022 Principles and Methodologies

• Tentative Table of Contents

PART I.      Polypharmacology as a New Branch of Pharmacology: Concept and Principles

Chapter 1.      Basics of Polypharmacology

            Introduce the basic concept and knowledge of polypharmacology, including the definition, principles, historical account, scope, branches, roles and responsibilities, and advantages and disadvantages of polypharmacology in separate subsections. Particular emphasis and explanations will be given to “Multitarget drugs”, and to the distinction among the concepts of Polypharmacology, designed Polypharmacology (multitarget drugs) and drug promiscuity (unintended Polypharmacology leading to drug toxicity).

Chapter 2.      Polypharmacology in Clinical Applications: Multitarget Multidrug-combination (MTMD-C)

            Describe the current status of applications of MTMD-C polypharmacology to various pathological entities in the clinical setting as well as in the preclinical situations. Illustrate the properties and strength of MTMD-C polypharmacology relative to the “Single-target, Single-drug” therapy and explicate the mechanisms of actions of MTMD-C.

Chapter 3.      Polypharmacology in Clinical Applications: Multitarget Multidrug-single-formulation (MTMD-SF)

Present the updated information on the use of MTMD-SF polypharmacology in the treatment of various diseases in patients, as compared to “Single-target, Single-drug” and MTMD-C therapies, their modes of actions, pharmacokinetics, efficacies and underlying mechanisms.

Chapter 4.      Polypharmacology in Clinical Applications: Multitarget Single-drug (MTSD)

Provide examples of MTSD polypharmacology in the treatment of various diseases in patients. Highlight its superior advantages and strengths in the therapeutic efficacy and safety profiles over other forms of pharmacological and polypharmacological therapies.  

Chapter 5.      Polypharmacology in Drug Discovery: Designed Epigenetic MTSD and Small-molecule MTSD

Describe the role of Polypharmacology in new drug discovery with focuses the rationally designed epigenetic MTSD and small-molecule MTSD, along with an introduction to natural product MTSD.  

Chapter 6.      Anti-cancer Polypharmacology

Introduce the use of Polypharmacology of different types (MTMD-C, MTMD-SF and MTSD) in the therapy of various types of cancer (lung cancer, breast cancer, leukemia, etc.) with real examples.

Chapter 7.      Cardiovascular Polypharmacology

Introduce the use of Polypharmacology of different types (MTMD-C, MTMD-SF and MTSD) in the treatment of cardiovascular disease (hypertension, coronary artery disease, arrhythmias, heart failure, ischemic stroke) with real examples.

Chapter 8.      Neuronal Polypharmacology

Introduce the use of Polypharmacology of different types (MTMD-C, MTMD-SF and MTSD) in the treatment of neuronal disease (Alzheimer's disease, Parkinson disease, epilepsy, etc.) with real examples.

Chapter 9.      Pulmonary Polypharmacology

Chapter 10.    Polypharmacology of Metabolic Disease

Chapter 11.    Polypharmacology of Infectious Disease

Introduce the use of Polypharmacology of different types (MTMD-C, MTMD-SF and MTSD) in the treatment of infectious disease (caused by bacteria, virus, parasite, etc.) with real examples.

Chapter 12.    Polypharmacology of Inflammation

Introduce the use of Polypharmacology of different types (MTMD-C, MTMD-SF and MTSD) in the treatment of inflammation with real examples.

Chapter 13.    Anti-psychotics Polypharmacology

Introduce the use of Polypharmacology of different types (MTMD-C, MTMD-SF and MTSD) in the treatment of various psychotic disorders (Schizophrenia, etc.) with real examples.

Chapter 14.    Anti-aging Polypharmacology

Introduce the use of Polypharmacology of different types (MTMD-C, MTMD-SF and MTSD), which aids to combat age-dependent physiological decline and the associated diseases with real examples.

Chapter 15.    Polypharmacology in Drug Repurposing

Introduce the use of Polypharmacology in drug repurposing (a highly efficient, time saving, low-cost and minimum risk of failure strategy and process of identifying new therapeutic uses for old/existing/available drugs).

Chapter 16.    Polypharmacology and Unintended Drug Promiscuity

Introduce the use of Polypharmacology in unintended drug promiscuity of old/existing/available drugs or lack of desired target specificity that can cause side-effects and toxicity in the clinical applications of the drugs.

Chapter 17.    Polypharmacology Pharmacokinetics

Introduce the complex process of absorption, distribution, metabolism, and excretion of Polypharmacology drugs in the human body. Describe the differences of the pharmacokinetic processes between Polypharmacology drugs and regular single-target drugs.

Chapter 18.    The Future of Polypharmacology

Provide the future perspectives of Polypharmacology as a new sub-discipline and a new strategy of drug discovery. Present the current difficulties in the applications of Polypharmacology to drug discovery and clinical therapy of human diseases and foresee the possible new challenges in the future development of Polypharmacology. Give my opinions to spark inspiration for new drug discovery projects.

PART II.     Polypharmacology in New Drug Development: Strategies and Protocols

Chapter 1.      Designed MTSD Discovery Process

Introduce the general process of drug discovery using the USA-FDA version as an example. Describe the step-by-step planning for rational “Multitarget Single-drug (MTSD)” discovery.

Chapter 2.      Designed MTSD Discovery Strategies

Introduce the currently available strategies of designed MTSD discovery and provide the rationales and considerations for choosing an appropriate strategy from the pool (experimental approaches vs. computational approaches; molecular docking approaches vs. molecular scaffold approaches; genomic approaches vs. epigenomic approaches; expression-based approaches vs. phenotype-based approaches; fragment-based approaches vs. molecular hybridization approaches, etc.), for the development of drugs for the treatment of a specific human disease of interest

Chapter 3.      Designed MTSD Discovery Technologies

Introduce the state-of-the-art technologies applicable to the designed MTSD discovery; compare the applicability and advantages of different technologies; and provide the rationales and considerations for choosing an appropriate technology for the development of medicines for the treatment of a specific human disease of interest.

Chapter 4.      Designed MTSD Discovery Databases

Introduce the databases for in silico approaches for the designed MTSD discovery; compare the applicability and advantages of over 30 different drug-discovery-relevant databases; and provide the rationales and considerations for choosing proper databases for a specific drug-discovery project.

Chapter 5.      Designed MTSD Target Deconvolution

Provide the step-by-step procedures for deconvolution/identification of designed MTSD targets with real examples.

Chapter 6.      Designed MTSD Target Validation

Describe the step-by-step procedures for target validation of designed MTSD with real examples.

Chapter 7.      Designed MTSD Lead Identification and Optimization

Describe the step-by-step procedures for lead identification and optimization of designed MTSD with real examples.

Chapter 8.      Designed MTSD Discovery Protocols

Describe the step-by-step protocols from A to Z for designed MTSD discovery.

Chapter 9.      Natural Products in MTSD Discovery

Introduce the basic principles and practical methodologies for MTSD discovery from natural products with a focus on phytochemicals.

Chapter 10.    Polypharmacology Procedures for Drug Repurposing

Introduce the fundamental principles and practical methodologies of Polypharmacology for the repurposing of old/existing/available drugs.

Chapter 11.    Polypharmacology Procedures for Drug Promiscuity Discovery

Introduce the fundamental principles and practical methodologies of Polypharmacology for the discovery of promiscuity of old/existing/available drugs..

Provides comprehensive, in-depth mechanisms behind the knowledge and methodology of Polypharmacology

Emphasis on rationally designed Polypharmacology or “multi-target, single-drug (MTSD)” pharmacology

Contains a wide collection of the state-of-the-art Polypharmacology technologies