|
| |
|
Case Studies |
|
|
Case Study 1
A
private mid-sized biotech company with 250 employees and an internal
medicinal chemistry department approached MedChem Partners to help them in
their drug discovery efforts. To facilitate in vivo work, the company needed
to have stable isotope derivatives of several lead compounds prepared, but
did not have the internal resources for the task.
The
company engaged MedChem Partners to prepare the stable isotope analogues and
MedChem Partners was able to assess the chemistry, quote a price and begin
chemistry within two weeks.
The two
compounds were delivered rapidly and in high purity, which allowed the
timely completion of the in vivo work. Based on quality of the work, the
company then retained MedChem Partners to expand on the project and make a
small library of compounds for SAR and testing.
MedChem
Partners and the company entered into an FTE relationship for the ongoing
iterative production of small libraries to develop back-up compounds to the
leads currently under development.
|
|
Case Study 2
Company
X is a pre-funding stage start-up based in a university incubator. The
company has two compound hits, which work as novel antibiotics in the
initial screen. The company does not have the internal resources nor the
experience to develop these candidates.
MedChem
Partners reviewed all of the data and worked with company X to prepare a
comprehensive plan for development of the two hit compounds. The plan
included a strategy for primary and secondary in vitro assays, preliminary
eADME work and in vivo testing. The compounds were ranked according to the
established selection criteria. In addition, MedChem Partners addressed the
patent strategy and developed a chemistry route that allowed for rapid
generation of analogs for SAR and optimization of PK/PD properties.
MedChem
Partners prepared a small library of compounds to explore the SAR around the
initial hits. Based on the information generated from this initial data
set, a second library was designed to optimize for biological activity and
solubility.
In
addition to this project, MedChem Partners worked with Company X to prepare
the due diligence scientific plan and presentations required for the initial
round of financing.
|
Case Study 3
A small
biotech with seed funding and a novel application for a known compound
retained MedChem Partners to help with the development of the new
indication.
The
Company wanted to begin lead optimization on the compound right away,
however, following the advice of MedChem Partners, an initial assessment of
the program was undertaken. The assessment revealed that the initial
compound's synthesis was problematic, there was very little IP space, and
the compound contained several potentially toxic functionalities. MedChem
Partners suggested an alternate structure which was easy to synthesize from
commercially available advanced intermediates, readily functionalized, and
did not possess the liabilities of the original core structure.
MedChem
Partners prepared a small library based on the new structure and found one
compound which was equipotent to the initial lead compound.
Based on
the positive results, MedChem Partners was hired to expand on the original
hit compound and continue lead optimization on the new core structure
|
Case Study 4
An
academic laboratory at a major university had discovered a novel therapeutic
target and found several weak hits in a high throughput screen. Based on
their early successes, they were encouraged to initiate a drug discovery
program to develop novel therapeutics against this target. The initial HTS
hits showed activity against the desired target in both enzyme and cell
based assays. The researchers were interested in applying for internal
university funding to initiate a medicinal chemistry hit-to-lead
optimization program.
MedChem
Partners worked with the academic group to create a comprehensive medicinal
chemistry development plan including: ranking of hits, weeding out of
potentially problematic structures, initial substructure patent searching,
designing a synthetic route for the core structures and a plan for rapid
analog generation. In addition, MedChem Partners presented the proposal to
the university funding chair, and assisted the academic researchers
defending the project.
The
proposal was funded by the university and MedChem Partners was retained in
an FTE relationship to implement the medicinal chemistry plan and help guide
the program forward. MedChem Partners designed and validated the synthesis
of the core structures and prepared several focused libraries to define the
SAR of these series. Several iterative rounds of medicinal chemistry and
screening were performed until the defined program milestones were reached.
This
program continues to move forward with the ultimate goal of finding angel or
venture funding to spin out as start-up.
MedChem
Partners continues to manage and implement the medicinal chemistry for this
project as well as assisting in the preparation of due diligence reports and
in the funding process as needed. |
|
|