Case Studies

Enabling Better Science
Through Innovation

Case Study 1

Logistics, Compound Management and Profiling One of MedChem Partners’ clients became semi-virtual with laboratory space dedicated only to biology research. The client approached MedChem Partners for help with compound storage, shipping, QC and other logistics related services. We designed a customized logistics solution which included compound storage at -80° C, inventory management, and shipping of solid or solution samples. The client’s initial need for compound storage and shipping quickly expanded to include QC of samples, profiling of samples for solubility and stability as needed and preparation of CoA documents to support testing. MedChem Partners has been providing logistics, compound management and profiling to this client for over 10 years.

Case Study 2

Compound Characterization and Preparation of CoA Documents One of MedChem Partners’ clients urgently needed CoA documentation for compounds that were going into an in vivo study. In addition to standard in- house analytical techniques such as LC/MS and ¹H NMR spectroscopy, the client also requested Karl Fischer, elemental analysis and FT/IR. MedChem Partners was able to co-ordinate the in-house and outsourced analysis and prepare the CoA documents within 3 days. Currently, MedChem Partners offers a variety of analysis either in-house or through outsources partners. Examples of analysis are: LC/MS and NMR spectroscopy elemental, moisture content, ash, UV/VIS and FT/IR, heavy metal panel, residual metal analysis, melting point, DLS, zeta potential, etc

Case Study 3

Synthesis of Stable Label Lipids A large pharma approached MedChem Partners with a request for an urgent synthesis of several stable label lipid reference compounds to be used in a bioanalytical study. The study was already scheduled and was being held by the lack of the internal standards. MedChem Partners prioritized this project and worked with the client’s internal DMPK group to accomplish technology transfer and initiate the synthesis. As the project unfolded, it became clear that the synthesis of one of the compounds was proving more challenging than expected and most likely will not be accomplished within the strict timeline. MedChem Partners worked with the client to identify a suitable replacement for this reference standard and initiate the synthesis of the new target within a week of defining the structure with the client. All reference standards were prepared within the required timeframe. This client continues to work with MedChem Partners for the synthesis of all stable label reference compounds

Case Study 4

Synthesis and Analysis of Feed Additives A virtual company contracted MedChem Partners to reproduce and scale the synthesis of several organic complexes of iron (III) that were used as feed additives for poultry. The original synthetic procedure was performed in academia and was unoptimized. MedChem partners undertook the project and optimized the procedure for yield and ease of product isolation. Following the successful optimization, MedChem Partners proceeded to further develop the procedure so that production could be scaled to produce the target compound on 1 kg scale. In addition, we worked with a process lab to transfer the technology and produce the target compound on multi kg scale. The client has since retained MedChem Partners to design and synthesize novel organic iron complexes with improved biological activity. On behalf of the client, MedChem Partners also coordinates all the testing for the product lots of the original iron (III) organic complex, which is currently under review for approval as an animal food additive in Europe. In addition, MedChem Partners is working with regulatory consultants in Europe and the US to define the product specifications.

Case Study 5

Functionalization of Stainless Steel Surfaces: A client approached MedChem Partners with a request to functionalize the surface of a stainless steel device using a super hydrophobic coating. MedChem Partners leveraged its experience in surface chemistry and modified several literature procedures in order to accomplish the task. MedChem Partners experimented with several methods of etching and surface preparation to identify the best method for the substrate, then attached an activated polyflourinated hydrocarbon to the surface and measured the contact angle and sliding angle of water on the surface. After identifying the best procedure for the substrate, MedChem Partners constructed a flow system to fully coat the interior of the metal framework and proceeded to functionalize the entire device. The resulting device met all the criteria of the client and the procedure was transferred to the client for scale up and production.

Case Study 6

Preparation of Drug Polymer Conjuates MedChem Partners was approached by a client to conjugate a cytotoxic drug to a dextran polymer backbone. Since the client’s current CRO that prepared the dextran was uncomfortable using the cytotoxic drug, the client engaged MedChem Partners to perform the synthesis. MedChem Partners successfully prepared several variants of the drug-polymer conjugate with different loading ratios and analyzed the final product for loading ratio and free drug. The client is currently working with MedChem Partners to prepare similar constructs with other drugs.

Case Study 7

Consulting for Scale Up: MedChem Partners was engaged by a client with a program in late development to help as a consultant on an ongoing scale up of material for toxicology testing and to prepare for GMP production. MedChem Partners helped the client working through multiple issues with the scale up and purity of the compound. In addition, MedChem Partners assisted in salt screening and polymorph problems associated with the different salt forms. Ultimately, the scale up CRO proved to be unsuitable for GMP production of the final tox lot and MedChem Partners helped the company find a new scale up partner and transition the process from one CRO to the other. In addition, MedChem Partners helped with the identification and and testing of several metabolites that were discovered, as well as, with CMC documentation and formulation issues. MedChem Partners also worked with the client’s patent attorney to document the compounds and the process and obtain a composition of matter patent, a process patent and a use patent for the candidate compounds.

Case Study 8

Optimization of Hit Compounds A pre-funding stage start-up based in a university incubator approached MedChem Partners with a request to prepare a comprehensive medicinal chemistry plan for the optimization of two hit compounds. After reviewing the data, MedChem Partners prepared the plan that 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 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, MedChem Partners worked with the client to prepare the due diligence scientific plan and presentations required for the initial round of financing.