Enabling Unbounded Possibilities - RSD
Transcript of Enabling Unbounded Possibilities - RSD
WuXi RSD Leadership:
Steve Yang
WuXi RSD Business Development:
US: Declan Ryan
EU: Dave Madge
Israel: Dana Yarden
Japan: Yan Zhu
Korea: Suk Young Cho
China: Marcher Xu
Enabling Unbounded Possibilities
The WuXi AppTec Research Service Division (RSD) aims at
providing superior support to our partners and promoting
efficiency and collaboration between WuXi’s business
units. RSD combines WuXi’s capability and technology
platform in chemistry, biology, oncology, and immunology
to provide open access and integrated service for drug
discovery and research. The services include in the new
RSD are the International Discovery Service Unit (IDSU),
the Chemistry Service Unit (CSU), the Oncology-
Immunology Unit, the Core Analytical Services Unit (CAS),
the Biology Unit (which includes HTS, in vitro screening,
infectious diseases, neurosciences, fibrosis, cardiovascular
and metabolic diseases), Crelux and newly acquired HD
Biosciences (HDB). This new integration will provide closer
points of contacts for our partners and discovery teams,
streamline the exceptional services offered across our
platform, and enhance efficiency and productivity to drug
discovery. We will focus on boosting our scientific
capabilities and leading technology development to
maintain WuXi’s industry leading position in technology
and research service. We aim to provide outstanding
service to our existing partners and to our broader
discovery community!
Steve Yang, Ph.D.
Chief Business Officer EVP & Head of RSD
International Discovery Service Unit
(IDSU)
Med. Chem. design solutions
Project management
Deliver preclinical candidates
Chemistry Service Unit (CSU)
Speed and quality syntheses
Shorten synthesis cycle time
Core Analytical Services Unit
(CAS)
Analytical testing and release
High throughput purification
SFC large scale chiral
separation
Impurity isolation and
identification
Natural products
Biology Unit
HTS and novel libraries
In vitro screening
platform
General pharmacology
Infectious disease
platform
Specialty models
including NASH
Crelux
High quality protein
production
Fragment screening
and biophysical hit
finding
X-ray crystallography
Oncology-Immunology Unit
CRISPR, targeted oncology
(PDX), immuno-oncology,
translational oncology
Immunology Center
Autoimmune and
inflammatory diseases
Comprehensive R&D enabling capability
RSD integrated platforms enable anyone or any company to discover and develop new drugs and products benefit to
patients. RSD services deliver extraordinary performance and an unwavering focus on customer satisfaction.
Target validation, CRISPR
Protein production
HTS, FBDD
X-ray crystallography
Biophysical analytics
CADD
In vitro efficacy & MoA
In vivo efficacy
PK/PD analysis
In vitro SAR support
Selectivity panel
Cell panel
In vivo target engagement
In vivo pharmacology
hERG, other safety profiling
services
Ligand binding
Receptor profiling
Additional in vitro and in vivo characterization
PDX
Tumor TILs
Biomarkers
CAP-certified FACS, pathology,
molecular testing
R&D Biological Science Chemistry
Reference compounds
Arrays, Libraries, DELs
Unique scaffolds, building blocks
DNA-Encoded Libraries
Customized screening decks
SAR generation
Molecule design
Building blocks
Optimization of hits and
leads
Data interpretation
Candidate selection
Scale up of candidates for
preclinical studies
Synthetic optimization of
candidates
Metabolic and impurity
identification synthesis
Hit-to-lead
Lead
Optimization
Pre-clinical
Target-to-hit
Clinical I - III
Commercial
HD Biosciences (HDB)
Biology-focused
preclinical drug
discovery
Drug target validation
HTS, H-T-L and LO
program support
Efficacy PK/PD,
disease models
IDSU
Oncology
Immunology
CSU CAS
Biology Crelux HDB
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
A number of historical milestones characterize RSD’s
journey from regional individual testing services to
integrated platforms and massive capacity that enable us
to provide outstanding and cost-effective services to help
our global clients tackle challenges in their drug discovery
process. Throughout the past decade, we have introduced
new testing technologies, animal models, libraries and
other chemistry and biology services through a steady
flow of innovations, expansions and acquisitions.
A steady flow of innovations and portfolio expansions
Benefits of Partnering with WuXi AppTec RSD
■ Track record of leadership and excellence in contract research
■ A broad and integrated portfolio of discovery services and seamless transition development services
■ >5,000 scientists across integrated chemistry and biology platform
■ Fast turnaround, comprehensive services, cost-effective solutions and quality results
■ Global footprint with operations in North America, Asia and Europe
■ Established stringent policies and procedures for IP protection
Leadership and excellence in contract research
AAALAC accredited
SPF animal facility
Acquired Crelux
GLP-certified
hERG testing
Scale-up facility
for peptide synthesis
Launched
OncoWuXi database
Immunology Core
Supported delivery
of >60 preclinical drug
candidates
Novel technologies -
CRISPR, PDX, & CDX
Acquired HD
Biosciences
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
The Chemistry Service Unit (CSU) is led by an experienced
scientific leadership team staffed with over 1,300 synthetic
and analytical/purification chemists. Services by CSU range
from custom synthesis of client-directed molecules and
libraries to WuXi designed templates. Our focus on
technology and continued innovation allows us to offer
specialized services in peptides, nucleosides, fluorine
chemistry and natural products, all led by experts of the
respective fields.
Synthesis with speed and quality
WuXi-designed templates/template libraries.
Extensive access to reagents and components through
WuXi LabNetwork.
Compound collection management including storage,
registration, distribution, etc.
Impurity isolation, identification and structure
assignment/confirmation.
Natural product extracts or purified natural product
sourcing, purifications, QA/QC and structure elucidation.
Snapshot of Accomplishments
>17 years of experience in route design and synthesis
>1,000 clients worldwide
>3 million compounds delivered, >20,000 each year
>25,000 reagents plus 8,000+ novel building blocks in
stock
>95% on-time delivery rate and short cycle time
20-30% client synthetic routes re-designed by CSU
CSU Services
Synthetic
chemistryCatalog
reagents
Analytical
services
Peptide
services
Building block
synthesis
Library synthesis
Custom synthesis
Scale up synthesis
Route scouting
Discovery-process
chemistry (DPC)
Templates
Reagent service
Compound
management
Chiral separations
Impurity analysis
Natural products
Non-GMP
peptide synthesis
GMP facility in
2017
CSU Service
Capabilities
Support for early-stage
research programs
Rapid scale-up for late-
stage needs
Discovery process chemistry
(DPC)
Combination of strong
discovery chemistry
experience
Strong route scouting
capability
Catalog
>3,000 templates developed
>14,000 unique scaffolds and
building blocks in stock
104K screening compounds
Library synthesis
Rapid production
Diverse chemistries
Discovery scale & rapid scale-up
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
Enables discovery stage of drug research
The International Discovery Service Unit (IDSU) is WuXi’s
solution to address our industry’s drug discovery
challenges through expertise in medicinal chemistry and
program management. We collaborate closely with our
international customers ranging from pharma and biotech
to academia to rapidly advance programs towards key
inflection points and milestones by leveraging
IDSU’s peer-recognized expertise and WuXi’s
integrated platform from hit identification to preclinical
candidate selection and beyond. With some of the
industry’s finest and most experienced medicinal
chemists at WuXi, we aspire to become the partner-of-
choice in externalized solutions to enable advancement
of programs in ways that are both smarter and faster.
Structural
Biology &
Computational
Synthetic
Chemistry
Safety Assessment
& Toxicology
ADME &
DMPK
In Vitro Biology
& In Vivo Pharmacology
Medicinal
Chemistry
Multiple biology screening
platforms
HTS, component collection
Electrophysiology
Biophysical characterization
Oncology, immuno-oncology,
immunology core, infectious
diseases, neuroscience & CV/MED
Translational models
Genomic Center (CLIA-certified)
Biomarkers
Rodents to NHPs
Discovery to IND-
enabling
Metabolite ID
Radiolabeled studies
>2,700 chemists
Discovery to candidate
selection & scale-up
Radiolabel synthesis
Protein crystallography
FBDD, SBDD
Modeling &
Chemoinformatics
Non-GLP and GLP
Toxicokinetics &
bioanalytical
Pathology
Leveraging WuXi Integrated Discovery Capability
Target
to
hit
Hit
to
leadPhase I Phase IIIPhase II
Submission
& launch
Lead
optimizationPreclinical
Snapshot of Accomplishments
>113,000 compounds delivered in
2017
>190 clients globally and >80%
from biotech and non-profit
organizations
34 publications in 2017
74 patent applications with WuXi
inventors
27 preclinical candidates (PCCs)
delivered in 2017
1st FDA-approved drug from
WuXi integrated platform
Partnering with IDSU
Collaborative. Having delivered 27 preclinical candidates in 2017 for our partners, we understand the unique challenges
and needs of each program. We work closely with partners to establish strategy, customize resources and guide project
execution to deliver on goals.
China Platform PartnerWuXi’s IDSU Team
Efficient. We provide our customers with access to WuXi’s best-in-class, fully integrated drug discovery and development
platform to seamlessly progress programs from target through to preclinical candidate selection and beyond.
Execution of
HTS & chemistry
in vitro & in vivo biology
DMPK & formulation
safety assessment
Medicinal chemistry
project execution
program management
Disease biology
target of interest
in-house expertise
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
Provide high quality integrated analytical services in a rapid & cost saving manner
The Core Analytical Services Unit (CAS) is led by a
dedicated and knowledgeable team with extensive
experience. Our focus on technology and continued
innovation allows us to offer specialized services in chiral
separation, high-throughput purification, physiochemical
property determination, and impurity isolation and
identification to our clients, and to meet their needs for
accurate and high quality data analysis on tight budget.
The CAS Unit is equipped with best-in-class automated
instruments to provide extensive GMP and non-GMP
conditions in both small and large scales.
SFC and/or HPLC chiral separation (mg to multi kg)
Regulated Analytical Research Services (ARS) for Drug
Development
High-throughput purification (500,000-700,000 compounds
annually)
Structure confirmation/elucidation (HRMS, 1D/2D NMR)
Physicochemical property determination (pKa, LogP/LogD,
thermodynamic and kinetic solubility, concentration)
Natural products extraction, purification, structure
identification and quality analysis
Isolation and structure elucidation for impurities of
regulatory starting materials, intermediates, APIs and drug
products.
Capability to purify /
characterize 500,000
compounds
MS and UV triggered Prep
HPLC fraction collection
Standard LC-UV-ELSD-MS
platform for QC of isolated
compound
Physiochemical properties: pKa,
LogD/LogP, thermodynamic and
kinetic solubility, etc.
Structure confirmation/elucidation Drug substance services
Drug product services
Stability studies
Reference material
standardization
Impurity isolation and
structure elucidation
High purity single compound
as reference
Most major natural product
classes covered in CAS Library,
~16% novel . (Non-exclusive
basis )
Bioassay guided isolation
Quality analysis of crude or
enriched extracts
Large scale single compound
extraction and isolation.
Major Services
for Natural
Products
Chiral
Separation
Services
Regulated
Analytical
Research
Services
High-
throughput
Purification
Physiochemical
Property
Determination
SFC/HPLC chiral separation
Separation method
development
Milligram and multi-kg scale
separation
ee Determination
Pure enantiomer racemization
study
Isolation of impurities/by-
products
Process Chemistry
Discovery Chemistry
Core Analytical Services Unit (CAS)
Integrated Analytical Services
Dedicated to Provide Analytical, Purification and Structure Elucidation Services
CAS
Tianjin
WuhanShanghai
CHINA
Snapshot of Chiral Separation Accomplishments
■ 14 sets analytical SFC, two equipped with MS detector
■ 12 sets semi-preparative SFC (flow rate 70-80 ml/min) equipped
with 2.5cm and 3cm columns
■ 11 sets prep-SFC instruments (flow rate 200-350 ml/min) equipped
with 5cm columns
■ 130 sets semi-prep and prep-HPLC to purify samples from mg to
multi-kg scales
■ Centralized CO2 delivery system with two 2,000-liter tanks
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
End-to-end service and solution to enable cancer drug discovery
Part of the Oncology and Immunology Unit, WuXi
Oncology team works efficiently with partners to enable
cancer drug discovery through our leading oncology and
immuno-oncology service capabilities. We provide a wide
panel of in vivo tumor model systems including human
cancer cell line-derived xenograft (CDX) models, murine
syngeneic tumor models/humanized models, and patient-
derived xenograft (PDX) models with in-depth genomic
characterization. We have established a comprehensive
immune profiling platform including TILs analysis, IHC
and TCR repertoire to advance immune-oncology
discovery. Our CRISPR screening and surrogate
antibodies can offer target validation service. The
oncology topnotch team has extensive experience in
IND-enabling studies for both FDA and CFDA filing as
either standalone or integrated drug discovery
programs, plus clinical biomarker service to support
clinical trials.
Oncology Platforms
Services
Solutions
>340 scientists, 70% with
MS/PhD
AAALAC credited SPF
animal facility
>6,000 IVC-cages capacity in
SPF barrier
WuXi Oncology Capabilities
TI/TS LO/TS IND/TS Clinical/Beyond
Medicinal Chemistry Toxicology cGMP Biology
Biologics WuXi NextCODE CDx Analytics
DMPK Clinical Trial CMC Commercial
Enable
Oncology Platforms from Drug Discovery to Translational Science
Biomarker discovery
o 18-color FACS-based analysis &
sorting
o Pathology lab
o Multiplexed IHC
Clinical Biomarker Services
o IHC, FISH, DISH, FACS
o CAP accreditation and GCP
compliance
CRISPR library in vitro & in vivo screening
o 18,000 genes
o Customized library
KO/KI of target genes
In vitro cancer biology
Xenograft Models
o >180 cell- linederived xenograft
(CDX) models
o 27 orthotropic models
o >1,000 patient-derived
xenograft (PDX) models
o SOC and genomic profiling
o Pathology services
54 syngeneic models
o Validated with checkpoint
inhibitors
o Immune profiling capability
o Humanized models
CRISPR/Cas9
Discovery &
Clinical
Biomarkers
Immuno-
Oncology
Oncology
>1,500 tumor models
Full annotation
o >3,000 growth curves
o >2,800 histology images
o >250 SOC studies
o >800 WES, CNV, Microarray & RNAseq
OncoWuXi Database
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
Efficacy and MoA study to facilitate immunotherapy drug discovery
Part of the Oncology and Immunology Unit, WuXi
Immunology Center is built to provide a comprehensive
open platform for immunological service of preclinical and
clinical studies, and to facilitate immunotherapy drug
discovery in cancer, autoimmune and inflammatory
diseases. Led by a group of US and European trained
immunologists, the team primarily serves clients’ needs for
efficacy and in depth mechanism of action (MoA) studies
by utilizing our cancer immunology platform, autoimmune
& inflammatory animal models, and biomarker detection
services. Our pathology lab and flow cytometry lab are
equipped with best-in-class automated instruments and
set up to follow GCP compliance and CAP regulation.
Immunology Center Services
In Vivo ModelsIn Vitro/Ex Vivo
Immunology
Flow Cytometry
Core
Surface &
intracellular
markers
Pre-clinical &
clinical studies
GCP/CAP
compliance
Biomarker services
Histology Core
Autoimmune
diseases,
inflammatory
animal models
Cancer
immunology
platform
Cell-based
biomarkers (flow-
cytometry lab)
Lab with GCP
compliance & CAP
accreditation
Soluble biomarkers (ELISA, Luminex,
CBA, MSD)
Tissue-based biomarkers
(pathology lab)
Integrated
Immunology
Platform
Immunology Center Capability
Snapshot of Accomplishments
■ >100 validated biomarkers
■ Laboratories with GCP compliance and CAP accreditation
■ Top flow cytometry service lab among CROs
■ Combination immunotherapy evaluation
IHC, FISH, DDISH
Pre-clinical &
clinical studies
GCP/CAP
compliance
Biomarker services
Immune cell
functions
Cytokines/
chemokines
Adoptive T cell
therapy
Adoptive T cell
therapy
Autoimmune &
inflammatory
diseases
Cancer
immunotherapy
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
An open access biology platform for global drug innovation
The Biology Unit offers plate-based screening services
including HTS, SAR screening support, compound
selectivity and early safety profiling, and cancer cell panel
profiling. In addition, we offer disease models and
therapeutic expertise in CNS and pain, infectious diseases,
cardiovascular diseases, metabolic disorders
fibrotic diseases. The 310+ membered team is
composed of 11% PhD, 54% MSc, and led by 14
seasoned scientific leaders with an average of 15
years of R&D experience in US, Canada, and UK.
>43,000 sq ft of Biology Labs, AAALAC-
accredited SPF animal facility
>250 global partners
>40 drug candidates delivered in 2008-2014
through integrated team effort
1st GLP-certified hERG testing; CAP-certified
molecular testing Lab (clinical virology)
Stand alone services
Integrated programs
HTS & novel screening libraries
Broad therapeutic area coverage
In vitro & in vivo pharmacology
Structural biology Established in 2015
Broad industry experiences
MoA
HTS & novel screening libraries
Assay development
>10 orthogonal biophysical assays for screening & characterization
Close to 200 targets ready for complex structure solution with client ligands
XPRESS, XPEDITE, XPERT services
100s of structures, greater than 15 target classes, small molecules, antibody structures
>80 global partners (pharma, biotech, academic institutes)
Global leader in crystallography & biophysical compound validation
Rapid, high quality protein production
Biophysical assays & screening
Structural biology for difficult targets
FBDD
Global Biology Footprint with Global Centers of Excellence
Snapshot of Accomplishments
>250 global collaborators including 14 partners from top 20
pharmaceutical companies
>40 drug candidates delivered in 2008-2014 through
integrated platforms
1st GLP-certified hERG testing; CAP-certified FACS, pathology
and molecular testing Lab (clinical virology)
Snapshot of Capabilities
~340 experienced scientists in in vivo and in vitro biology
13 Senior managers trained in US & Canada, 10 with >15 years
R&D experience
HTS services in US, Europe and China to support global clients
43,000 sq ft biology labs and AAALAC-accredited animal
facility
Partner
R&D Idea
New Target
/Biology
/Mechanism
In Vitro Assay
Development
384 & 1536
Hit Validation
&
Series
Expansion
Hit to Lead
Optimization
Lead
Optimization
to PCC
HTS & Hit
Confirmation
One Stop Shop at WuXi – Integrated Discovery Roadmap
The Only Comprehensive CRO Offers HTS Services in US, EU, & China
US: Assay Design & Screening EU: ProteinChina: Assay Development, Transfer
& Screening
Bio
log
y
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
Global leader in structural biology and biophysical solutions
Crelux, founded in 2005 at the Innovation & Startup
Center for Biotechnology (IZB) in Martinsried, Germany, is
a global leader in structure-based drug discovery. Crelux
has been providing the drug discovery industry with highly
individualized and efficient solutions to inform and
accelerate their programs for more than a decade. Crelux
provides a number of customized services to support hit-
finding, conformational analysis and lead optimization,
including protein production, biophysical assays,
fragment screening, and X-ray crystallography. The
acquisition represents a further step in the growing
European presence of WuXi AppTec and reaffirms
WuXi's strong commitment to better serving and
interacting with European customers. It provides a
solid foundation for WuXi to expand its integrated
drug discovery services within Europe.
Hit Finding Validation Optimization
High Quality Proteins · FBDD · Biophysical Assays and Screening · X-ray Crystallography
STRUCTURE INFORMED DISCOVERY
Your discovery.
Our solutions.
>10 biophysical validation technologies
X-ray crystallography
of challenging targets
At Europe’s
#1 bio hub
>170 established targets for fast-track complex structures
Delivering Individualized Structure-Based Drug Discovery Solutions
Snapshot of Capabilities
High quality protein production
>10 Orthogonal biophysical assays and screening systems
>170 Targets ready for XPRESS complex structure solution with
client ligands
Fragment-based screening with >3,000-member novel fragment
library
Cryo-EM
Cell-based thermal shift assays (CETSA) for target engagement
Snapshot of Accomplishments
>200 New structures every year, across 30 or more protein
targets
Comprehensive coverage of target classes and therapeutic
modalities
Multiple drug discovery programs leading to launched products
supported with Crelux structural biology data
>80% Returning clients
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
Your world-class partner for accelerated drug discovery
HD Biosciences was founded in 2002 and is
headquartered in Shanghai, China with operating facilities
in Beijing, China and San Diego, USA. As a leading biology
and preclinical service provider, our plate-based
pharmacology, screening capability and AGMTM based
target validation are industry leading platforms with great
reputation. HD Biosciences also provides hit identification,
lead discovery, in vivo pharmacology and other related
services. During the past 14 years, HD Biosciences has
developed into a global company with wide recognition.
The business combination of WuXi AppTec and HD
Biosciences is an important step in strengthening
WuXi’s biology and preclinical service capability from
target validation to lead discovery and optimization,
improving and expanding WuXi’s open-access
enabling service platform. The combination of WuXi
AppTec and HD Biosciences will also provide additional
resources and space to take our biology focused
capabilities to the next level and to speed up the
growth of our business into a leading global player
within our sector. We will provide better services to our
current clients and expand services to WuXi’s global
customers.
Requirements
• Resources & Procurement
• Logistics
• Infrastructure and teams
• Team and specific expertise
• SOP driven process
Gaps &
common
challenges
• Infrastructure gap
• Team & expertise gap
• Technology gap
• Process gap
Shared practice
for solution
development
• Leadership identification & capability assessments, key to the solution
• Resources availability, conventional & alternatives, time line for procurement
• Expertise & infrastructure, internal and external; solutions for in house buildup, backup plan
• Process and PM, faster implementation with open communication & execution
• Mindset for continual improvement
Competitive
advantages at
HD Biosciences
• Talent team with track record
• Experience in running multiple programs & multiple clients
• Established structure with partners and clients in logistics/PM, IT/data support, etc.
• All established SOPs, EHS that compatible with industry standard
Key Elements and Gap Analysis Exercise: When a Collaboration Starts
Snapshot of Capabilities
Plate-based pharmacology with comprehensive assay technologies
and matching screening capability (SAR, HTS, profiling)
Advanced Gene Manipulation (AGMTM) platform featured by
CRISPR, AAV, shRNA for both in vitro and in vivo target validation
Tumor cell panel profiling on 1000+
cell lines supported by
proprietary database with genetic information
State-of-the-art facility with high end instrumentation providing
high throughput solution including RapidFire/ADDA, iQue, Biacore
8k, for bioanalytical and biomarker analysis
Comprehensive animal models covering Oncology, Immuno-
Oncology, Metabolic/liver diseases, and Inflammatory diseases, etc.
Snapshot of Accomplishments
Partners with all top 10 world largest pharma and biotech
Great reputation on scientific expertise & value delivery
20 million data points delivered annually from screening center
1,000+ assays developed for hit identification and lead discovery
50+ HTS campaigns launched in the past 3 years
50+ SAR/Hit Triage running in parallel throughout the years
Platforms & Services
to Accelerate
Drug Discovery
Process
Assay & Biology
ADME/SafetyHit to Lead &
Lead Discovery
Efficacy PK/PD Disease
Model
Drug Target
Validation
HD Biosciences Core Competences for Client’s Drug Development R&D
Target ID &
Discovery
Hit ID &
H2L
Lead ID &
Optimization
Safety &
Profiling
Preclinical &
IND
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities
Structural biology case study: in collaboration with a major pharma partner
Objective
An integrated Med. Chem. program to identify a potent and selective inhibitor for epigenetic target.
Biology Achievements
Repeated expression & purification of protein and optimized the purification protocol.
Obtained >120 co-crystal structures with >80% successful rate.
Analyzed co-crystal structures, crystal packing and biological data.
Deployed the structures to design novel targets and improve binding potency (200x), selectivity
(50x), and aqueous solubility.
Co-authors in publication.
Milestones
Demonstrated in vivo efficacy and studies. identified candidates that meet PCC profiles.
Completed in vivo toxicology experiments.
1.1 Å resolution
HCV: discovery of Elbasvir (NS5A inhibitor)
Scope of Partnership
Fully integrated program (Med. Chem., biological testing, DMPK) with WuXi designers.
Results
Key intellectual contributions by WuXi medicinal chemists leading to more than 10 patents
Med. Chem. designed by WuXi chemists
Biology contributed to nomination of 4 preclinical candidates (PCCs) including elbasvir (NCE)
Scientific and Medical Significance
1st Breakthrough Therapy to be designed in “China for the world”
For the patients, significant treatment for hard-to-treat HCV genotypes
Zepatier® : Breakthrough Therapy co-invented through Merck-WuXi partnership
Value to Merck
Full realization of an externalized discovery strategy leading to an approved drug
May 2008program initiation
Nov 2008In vivo PK at WuXi
May 2009
In vitro screens at WuXi
Jan 20101st PCC delivered
MK-4882
Oct 2010
FIH for
MK-4882
Dec 2010
2nd PCC delivered
MK-8742 (elbasvir)
Nov 2011
FIH for
MK-8742
Oct 2013
Breakthrough therapy designation
(elbasvir + grazoprevir)
Jan 2016
US and Canada approved Zepatier®
Computational
Structural
biology,
biology
Medicinal
chemistry
DMPK,
Tox,
process
Enabling Unbounded PossibilitiesEnabling Unbounded Possibilities