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Day 1 |
Day
2
| KEYNOTE
PRESENTATION |
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1:40 The Continuing Story of
Inhaled Insulin
Tim
Riley, Ph.D., Vice President of PEGylation Research,
Nektar Therapeutics
After 16 years of
development, the first inhaled insulin, Exubera, was
approved in January 2006 for meal time use by Type 1 and
Type 2 diabetics in both Europe and the US. The dry powder
product was a joint effort between Inhale Therapeutics
(now Nektar Therapeutics) and Pfizer. Exubera represents a
large number of technical firsts, and was widely preferred
over injections by diabetics who used it. In October 2007,
Pfizer stopped marketing the product because of poor
sales. This was the first time that a new product was
pulled from the market without any safety concerns. The
story of inhaled insulin continues as other companies move
their products to market. |
2:10 Engineering the
Pharmacology of Protein Therapeutics
Roberto
Mariani, Ph.D., Senior Scientist, Ambrx
The success of
modern drug discovery and development programs are highly
dependent on the ability to efficiently transition from
activities observed in "lead’ compounds to creation
of therapeutically relevant entities – molecules
possessing the appropriate (or competitive) efficacy,
safety and pharmacological profiles. In the case of small
molecule drugs, medicinal chemists are able to start from
an active lead scaffold and optimize the
structure-activity of candidates by drawing from an almost
limitless space of chemical diversity. Unfortunately, in
the case of protein leads, protein chemists are limited to
the optimization that can be performed with the set of
chemical groups present in the natural 20 amino acids.
While there are now a few examples of commercially
successful optimized or second generation protein products
utilizing the natural 20 amino acids, the ability to
incorporate novel amino acids (Protein Medicinal
Chemistry), especially those with chemo-selective
properties, provides new tools to optimize proteins such
as Growth Hormone, GCSF and Ifn-alpha.
2:40 Solutions Showcase (Sponsorship
Available)
3:10 Refreshment Break in
the Exhibit Hall
4:00 Recombinant Protein
Sequences with PEG-Like Properties for Half-Life
Extension
Volker Schellenberger, Ph.D.,
Vice President, Drug Discovery, Amunix, Inc.
The modification
of proteins with hydrophilic chemical polymers like PEG is
a validated approach to improve the pharmacokinetic
properties of many therapeutic proteins. However,
PEGylation requires an expensive conjugation step and it
typically leads to product mixtures resulting in complex
clean-up and characterization protocols. We developed
recombinant protein sequences (called rPEG) that share
many properties of PEG polymers: large hydrodynamic
radius, slow kidney filtration, low immunogenicity. These
rPEG sequences can be directly fused to most drug proteins
thus eliminating the need for chemical conjugation. Fusion
proteins between rPEG and several protein drugs were
manufactured in microbial hosts. These proteins closely
mimic the properties of PEG-conjugated proteins.
4:30 Use of Hesylation to
Improve Drug Characteristics, Such as Circulating
Half-life and Efficacy
Peter Vorstheim, Ph.D., Senior
Vice President, HESylation Technology, Fresenius Kabi
Deutschland GmbH
HESylation
utilises hydroxyethyl starch derivatives linked to drug
substances (e.g. proteins, peptides, oligonucleotides) in
order to modify the drug characteristics. This
modification enables the prolongation of the circulation
half-life by increasing the stability of the molecule, as
well as by reducing renal clearance, resulting in an
increased biological activity. Furthermore, HESylation
potentially alters the immunogenicity or allergenicity. By
varying different parameters, such as the molecular weight
or the number of hydroxyethyl groups of HES, a wide range
of HES drug conjugates can be customized. HESylation is
based on the extensive expertise of Fresenius Kabi in the
field of hydroxyethyl starch as the world’s largest
producer of HES. HES is a modified natural polymer that
has been widely used in clinical practice for decades as a
plasma volume expander. Consequently, it has an impressive
safety record.
5:00pm End of Day
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