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- An Overview of Drug Discovery and Development
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1. Rules and filters and their impact on success in chemical biology and drug discovery
- Dr. Christopher Lipinski
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2. Where did drugs come from?
- Dr. David Swinney
- Target Selection in Early Stage Drug Discovery
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3. G-Protein coupled receptors in drug discovery
- Dr. Mark Wigglesworth
-
4. Enzymology in drug discovery 1
- Prof. Robert Copeland
-
5. Enzymology in drug discovery 2
- Prof. Robert Copeland
-
6. Inhibiting protein-protein interactions 1
- Dr. Adrian Whitty
-
7. Inhibiting protein-protein interactions 2
- Dr. Adrian Whitty
- Key Drug Discovery Challenges in Major Therapeutic Areas
-
8. Current trends in antiviral drug development
- Prof. Dr. Erik De Clercq
-
9. The challenge of developing drugs for neglected parasitic diseases
- Prof. James Mckerrow
-
10. Is there a role for academia in drug discovery
- Dr. Adrian J. Ivinson
-
11. Key drug discovery challenges in cardiovascular medicine
- Dr. Dan Swerdlow
- Dr. Michael V. Holmes
- Methods of Hit Identification
-
12. Fragment-based lead discovery
- Dr. Daniel A. Erlanson
- Medicinal Chemistry and SAR
-
13. Hit to lead
- Dr. Michael Rafferty
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14. Prodrug strategies to overcome problems in drug therapy
- Prof. Jarkko Rautio
-
15. Deep ocean microorganisms yield mechanistically-novel anticancer agents
- Prof. William Fenical
- From Lead to Drug
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16. Biomarkers in drug development: potential use and challenges
- Dr. Abdel-Bassett Halim
- Case Studies in Drug Discovery
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17. Current concepts for the management of patients with osteoporosis
- Dr. Michael Lewiecki
-
19. Teixobactin kills pathogens without detectable resistance
- Prof. Kim Lewis
-
20. Discovery of schizophrenia drug targets from DISC1 mechanisms
- Prof. Atsushi Kamiya
- Archived Lectures *These may not cover the latest advances in the field
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21. CNS-drug design
- Prof. Quentin Smith
-
22. Imatinib as a paradigm of targeted cancer therapies
- Prof. Brian Druker
-
23. New and emerging treatments for osteoporosis
- Dr. Michael Lewiecki
-
24. Prodrugs and drug delivery
- Prof. Jarkko Rautio
Printable Handouts
Navigable Slide Index
- Introduction
- Outline
- Prodrug concept
- Examples
- Prodrug design
- Rationale for prodrug design (1)
- Rationale for prodrug design (2)
- Formulation and administration problems (1)
- Formulation and administration problems (2)
- Overcoming poor solubility
- Addition of non-ionizable polar functionality
- Addition of ionizable phosphate functionality
- Successful phosphate prodrugs (1)
- Successful phosphate prodrugs (2)
- Poor lipophilicity (1)
- Poor lipophilicity (2)
- Successful lipophilic prodrugs
- Problems of ester prodrugs
- Utilization of GI tract transporters
- Many antivirals are prodrugs
- Overcoming distribution problems
- Overcoming metabolism & excretion problems
- Overcoming toxicity problems (1)
- Overcoming toxicity problems (2)
- Prodrug prevalence
- Best selling prodrugs in 2009
- Summary
- Further reading
- Thank you
Topics Covered
- Prodrugs and drug delivery
- Prodrug concept and designing prodrugs
- Solving ADMET properties
- Prevalence, recent approvals and best-sellers
Talk Citation
Rautio, J. (2013, September 23). Prodrugs and drug delivery [Video file]. In The Biomedical & Life Sciences Collection, Henry Stewart Talks. Retrieved December 27, 2024, from https://doi.org/10.69645/HJTP9556.Export Citation (RIS)
Publication History
Financial Disclosures
- Prof. Jarkko Rautio has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.
A selection of talks on Pharmaceutical Sciences
Transcript
Please wait while the transcript is being prepared...
0:00
Hello, everyone, I'm
Professor Jarrko Rautio
from the School of Pharmacy
University of Eastern Finland.
The subject of my talk is prodrugs
and their role in drug delivery.
In general, prodrugs can provide
a means of solving drug delivery
challenges associated
with many new chemical
entities having larger and more
complex molecular structures.
In fact, prodrugs are
becoming an integral part
of the drug discovery
paradigm in some
large pharmaceutical companies.
Also, a number of
small biotech companies
have built around to design
an application of prodrugs
to improve their drug candidates.
I myself have a 15-year
experience with prodrugs,
and I have been working on several
various product applications
so far.
For example, in the early
stages of my research carrier,
I studied dermal prodrugs.
This was followed by research
on water soluble prodrugs
mostly on phosphates and then on
cytochrome p450 activated prodrugs,
which were targeted to the liver.
My most recent studies have focused
on sulphenamide prodrug approach
to increase the lipophilicity of a
very hydrophilic and basic quantity
in drug.
And we have also spent
quite a lot of time
with prodrugs which are designed
to take advantage of amino acid
transporters at the
blood-brain barrier
and to be taken up into the brain.
1:19
I have divided my
presentation into four parts.
First, I'm going to
tell what prodrugs are.
Then in the second part,
I'll show in one slide
the most common functional groups
and drugs amenable to prodrug
design as well as the most
common prodrug structures
for this functional groups.
Then the main part
of my presentation
will be dedicated to
prodrug examples that
have been approved for marketing.
These examples are
roughly divided based
on various problems or
barriers which have been
overcome in prodrug approaches.
Finally, at the end of my talk,
I'll show some prodrug statistics,
and I'm sure that the numbers
I'll show will surprise some.