ASSIGNMENT 1

OUR LADY OF FATIMA UNIVERISTY

COLLEGE OF PHARMACY
PMOC LEC

Drug Discovery and Drug product development

Answer the following. Cite your references

1. What are the Phases of Drug development?

The development of drugs begins with their discovery. The

identification of new drug is possible when new insights and
technology become accessible. Typically, researchers find
out new drug through new perspectives on a disease
process that allow researchers to construct a medicine to
DISCOVERY AND DEVELOPMENT counteract or prevent the effects of the disease. On this
phase, the process includes the identification of drug
candidates, synthesis, characterization, screening, and
assays for therapeutic efficacy. If a molecule achieves
faivourable findings in these investigations, it will begin the
process of drug development subsequent to clinical trials.

In the drug development process, pre-clinical research

entails evaluating a medicine's safety and efficacy in animal
models before concluding prospective human outcome. The
PRE CLINICAL RESEARCH appropriate regulatory authorities must also approve the
pre-clinical experiments. The regulatory authorities must
guarantee that trials are done in a safe and ethical manner
thus would give approval for only those drugs, which are,
confirm to be safe and effective. Preclinical trials test the
new drug on non-human subjects for efficacy, toxicity, and
pharmacokinetic (PK) information.

Before beginning clinical trials, drug developers must submit

INVESTIGATIONAL NEW DRUG PROCESS
an Investigational New Drug application to the FDA. In the
IND application, developers must include preclinical and
toxicity study data, drug manufacturing information, clinical
research protocols for studies to be conducted, previous
clinical research data (if any), and information about the
investigator/ developer.

Clinical trials are studies that are undertaken on individuals

CLINICAL RESEARCH (volunteers) to answer specific questions about the safety
and efficacy of medications, vaccines, other therapies, or
novel ways of using existing treatments. Clinical trials
adhere to a pre-determined study protocol designed by the
researcher, investigator, or manufacturer. The developers
will examine what they intend to accomplish for each of the
Clinical Research Phases.

Phase I: To determine the safety of the drug in humans and

to collect data on dose. Phase I trials also help to determine
the optimal way to give the medicine in order to minimize
toxicity and maximize therapeutic efficacy.

Phase II: To gather more safety information in order to

establish efficacy and side effects. This information will be
utilized to improve the Phase III study's design.

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of any adverse side effects. Long-term or rarer side effects
that may have gone undetected in Phase I and Phase II are
frequently recognized due to the larger number of patients in
Phase III. Phase III is when the majority of the safety data is
gathered.

The full information of a therapeutic molecule is expressed

in a New Drug Application (NDA). Its goal is to ensure that a
medicine is safe and effective in the people who will be
using it. In the NDA, a drug researcher must include all
FDA DRUG REVIEW information about a drug, from preclinical data to Phase 3
trial results. Developers must report on all reports and
investigations, data, and analysis. The company can finally
file to market the drug if the investigator provides sufficient
material from preclinical to clinical phases that demonstrate
the drug's safety and efficacy. The regulatory authority is
responsible for the scientific evaluation of the NDA or MAA.

When the FDA has approved a drug or device, Phase 4

POST-MARKET DRUG SAFETY MONITORING
studies are carried out. After the completion of clinical trials,
this is the process of monitoring the safety of medications
once they reach the market. The fundamental goal of PMS
is to find previously unrecognized adverse effects as well as
positive effects. Off-label drug use, orphan drug difficulties,
and issues in conducting international clinical trials in the
pediatric population are all important factors to consider.

References:
US Food & Drug Administration. (2018). The Drug Development Process. Retrieved from: https://www.fda.gov/patients/learn-
about-drug-and-device-approvals/drug-development-process

Deore, Amol & Dhumane, Jayprabha & Wagh, Rushikesh & Sonawane, Rushikesh. (2019). The Stages of Drug Discovery and
Development Process. Asian Journal of Pharmaceutical Research and Development. 7. 62-67.
https://10.22270/ajprd.v7i6.616. Retrieved from:
https://www.researchgate.net/publication/341097009_The_Stages_of_Drug_Discovery_and_Development_Process

Hughes, J. P., Rees, S., Kalindjian, S. B., & Philpott, K. L. (2011). Principles of early drug discovery. British journal of
pharmacology, 162(6), 1239–1249. https://doi.org/10.1111/j.1476-5381.2010.01127.x. Retrieved from:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3058157/

Mohs, R. C., & Greig, N. H. (2017). Drug discovery and development: Role of basic biological research. Alzheimer's &
dementia (New York, N. Y.), 3(4), 651–657. https://doi.org/10.1016/j.trci.2017.10.005
Retrieved from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5725284/
2. Give the importance of the physicochemical properties of drug on its mechanism of action in the body.

Physicochemical properties is the ability of a certain compound to elicit pharmacological effect related
to interactions with different media, influence of physical, chemical properties and molecular attributes. Its
parameters includes solubility, pH, temperature, conductivity, ionization, complexation, dissociation constant,
hydrogen bonding, surface activity, etc.
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Complete knowledge and understanding of physicochemical properties of the drug is important iorder
to determine the proper formulation, absorption, delivery method and mechanism of drug. Wherein the
physicochemical properties of drugs may dictate the fate of drugs, whether easily absorbed, distributed in the
body or do drug/protein binding producing its therapeutic effect effectively.

3. What is Lipinski’s rule of five?

To describe Lipinski’s rule of five, is a rule of thumb that characterizes a molecule's pharmacological capacity.
This rule assists in determining if a biologically active molecule has the chemical and physical characteristics
to be orally bioavailable. The Lipinski rule is based on molecular characteristics to predict pharmacokinetic
Reference:
drug qualities
Patel, such
K. (2018). as absorption, distribution,
Physicochemical Properties ofmetabolism, and excretion.
the drug. Retrieved from
https://www.slideshare.net/jaymaa/physicochemical-properties-of-drug

4. What is Pharmacodynamics?

Pharmacodynamics is the study of a drug's molecular, biochemical, and physiologic effects or actions. It is
derived from the Greek terms "pharmakon" meaning "drug" and "dynamikos" meaning "power." All drugs work
by interacting with biological structures or targets on a molecular level to modify how the target molecule
functions in relation to subsequent intermolecular interactions. Chemical interactions, receptor binding, and
post-receptor effects are examples of these interactions.
Reference:
Benet, L. Z., Hosey, C. M., Ursu, O., & Oprea, T. I. (2016). BDDCS, the Rule of 5 and drugability.
Advanced drug delivery reviews, 101, 89–98. https://doi.org/10.1016/j.addr.2016.05.007

5. Define the following

A. Receptor - Receptor, particle, for the most part a protein that gets signals for a cell. Little atoms, such as
hormones exterior the cell or moment flag-bearers interior the cell, tie firmly and particularly to their
receptors. Official could be a basic component in affecting a cellular reaction to a flag and is affected by a
cell’s capacity to specific, as it were certain receptor genes.
B. Agonist - Agonists are drugs or actually happening substances that actuate physiologic receptors, while
enemies are drugs that square those receptors. In this case, angiotensin II is an agonist at AT1 receptors,
and the antihypertensive AT1 drugs are antagonists.
C. Antagonist - A substance that acts against and blocks an activity. Adversary is the opposite of agonist.
Antagonists and agonists are key players within the chemistry of the human body and in pharmacology.
D. Enzyme - The biological forms that happen inside all living life forms are chemical responses, and
chemicals control most. Enzyme, a substance that acts as a catalyst in living life forms, controlling the rate
at which chemical responses continue without itself being modified within the process.

E. Down regulation - A decrease within the number of receptors on the surface of target cells, making the
cells less touchy to a hormone or another agent. For illustration, insulin receptors may be downregulated
in sort 2 diabetes.
F. Desensitization - Desensitization, moreover called Hyposensitization, treatment that endeavors to
dispense with unfavorably susceptible responses, as of feed fever or bronchial asthma, by a arrangement
of infusions in evaluated qualities of the substance to which the individual is delicate (e.g., dust, house
clean).
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References:

Cooper, J. A. (2018, November 23). Receptor. Encyclopedia Britannica.

https://www.britannica.com/science/receptor-nerve-ending

Stoppler, M.C. (2021, March 3). Medical Definition of

Agonits.https://www.medicinenet.com/agonist/definition.htm

Stoppler, M.C. (2021, March 29) Medical Definition of Antagonist.

https://www.medicinenet.com/antagonist/definition.htm

Britannica, T. Editors of Encyclopaedia (2019, December 5). Enzyme. Encyclopedia Britannica.

https://www.britannica.com/science/enzymeu

Davis, C.P. (2021, March 29) Medical definition of downregulation.

https://www.medicinenet.com/downregulation/definition.htm

Britannica, T. Editors of Encyclopaedia (1998, July 20). Desensitization. Encyclopedia Britannica.

https://www.britannica.com/science/desensitization-medicine

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