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Drug Discovery
Drug Discovery

Early Pharmacokinetics

Discovery DMPK is an essential part of drug discovery, as it is conducive to the evaluation of compound properties in the early stage, playing an important role in R&D efficiency improvement and risk reduction in later stages. Medicilon is one of the first CRO companies in China to offer discovery DMPK services. We have an experienced pharmacokinetic research team, as well as an advanced platform that provides fast and reliable early DMPK services for clients.

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Service
  • AbsorptionCaco-2 permeabilityTransmembrane transport tests(Caco-2, P-gp, BCRP, OATs/OCTs/OATPs, etc.)DistributionProtein binding: plasma, tissue, and microsomesWhole blood/plasma distribution testsMetabolismMetabolic stability:(Liver microsome stability tests, S9 stability tests, Hepatocyte metabolic stability tests, Plasma stability tests)Matric stability: plasma, tissue, and bufferIn vitro metabolite profiling and identification(Metabolite speculation, Metabolite confirmation; Estimation of metabolic pathways, Confirmation of metabolic pathways)Drug-drug interaction(DDI)Cytochrome P450 (CYP) inhibition (IC50 and TDI)P450 enzyme inductionEnzyme phenotyping: phase I and phase II enzymes (recombinant enzyme and chemical inhibition)Physicochemical properties (Lipophilicity, solubility tests)In vitro toxicity(hERG test, Mini-Ames)Rapid screening or IND support
Service Platform
  • The micromolecule analysis instrument platform represented by Sciex/Waters/Shimadzu ultra-high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) and Thermo Q Exactive HF-X quadrupole/ultra-high-field fourier transform ion trap high-resolution mass spectrometry  The macromolecule analysis instrument platform represented by the MSD high-throughput multi-protein detector, Luminex liquid-phase chip protein analysis system, the Gyrolab nano-upgraded microfluidic immunoassay workstation and the Applied Biosystems real-time fluorescent quantitative PCR system  The sample pretreatment platform represented by the Covaris AFA adaptive focused acoustics high-performance sample processing system, the KingFisher Flex automatic magnetic bead extraction and purification system, the Lysera high-efficiency sample crusher and the TurboVap high-speed sample concentrator  The sample management platform composed of Thermo/Panasonic ultra-low temperature refrigerators, the SensaTronics temperature monitoring system and the Watson LIMS laboratory information management software
Cases

Medicilon Assistant Jimincare's lgE Antibody Drug JYB1904 has been Approved for Clinical Trials.webp

Medicilon Assistant Jimincare's lgE Antibody Drug JYB1904 has been Approved for Clinical Trials

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ABM Therapeutics presented Medicilon with a commemorative trophy of our first candidate compound.webp

ABM Therapeutics presented Medicilon with a commemorative trophy of "our first candidate compound"

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Medicilon Won Praise and Awards From Many Partners.webp

Medicilon Won Praise and Awards From Many Partners

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FAQ
  • Why is Early DMPK Important?

    In 1991, up to 40% of failures in the clinical phase of new drug development were associated with drug DMPK properties; in 2000, the likelihood of late failure was dramatically reduced to less than 10% as major pharmaceutical companies shifted to early DMPK studies.

    (1) Early pharmacokinetic testing allows for a low-cost, short-term risk-benefit assessment of new drug development projects.

    (2) Guiding the processes from optimization of lead compounds to determination of preclinical drug candidates.

  • What are the Six Major Types of Early DMPK Studies?

     (1) Protein binding: plasma, brain tissue, microsomal protein, FBS; Erythrocyte /plasma partition ratio

     (2) Optimization permeability and transshipment: Caco - 2. MDCK - MDR1 / BCRP, OATs/OCTs/OATPs

     (3) In vitro metabolic DDI: P450 inhibited TDI, P450 induced /PXR, metabolic enzyme phenotype.

     (4) Metabolic stability: microsomes, S9, hepatocytes, plasma, whole blood

     (5) Metabolite Screening and Identification: in vitro, in vivo, and GSH Trapping

     (6) In vivo PK: rat, mouse, dog, monkey, pig, rabbit box/single administration

    --- IV/IJVC/SC/TD/IM/IP/PO/SL/IN/IVT

    --- Continuous cross/single point blood sampling

    --- BBB(homogenate /CSF), Tissue distribution excretion (BDC), in vivo DDI (ABT)


  • Can Medicilon Complete Preclinical DMPK Services?

    (1) 19+ years of accumulated experience.

    (2) Completing preclinical DMPK filing studies for about 20 new drugs per year.

    (3) In vivo PK screening of >2000 compounds per year.

    (4) One-stop service for PK/PD.

    (5) Antibody/ADC preclinical DMPK services.

    (6)Technical service solution for isotope drug metabolism research.

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