PKMS Knowledge Center

Pharmacokinetics and Mass Spectrometry Core Facility (PKMS) is a shared core resource facility in UM, and serves the scientific research community at UM and beyond with state-of-the-art expertise, methodology, and instrumentation. We are pleased to offer a complete PK service to your research projects with different options including collaboration, Fee-for-Service (FFS) and self-service. Please check our complete PK analysis service - from in vitro and in vivo drug discovery to bioanalysis and Mass spectrometry imaging.

Pharmacokinetics (PK) is the study of the time course of drug’s absorption, distribution, metabolism, and excretion (ADME), what the body interact with a drug, related to the movement of drug into, pass, and out of the body. In order for a drug to be effective in the body, enough of the active form must reach the target to elicit the desired effect. The compound with the best activity against the target enzyme or receptor may have very poor ADME characteristics such as metabolic instability or poor intestinal absorption. When choosing a lead candidate from multiple compounds, the activity of the drug in the efficacy screen must be balanced with acceptable ADME and stability characteristics. Pharmacokinetic studies with mass spectrometry bioanalysis can provide the quantitative information about the half-life of the administrated compound from in vitro and in vivo test, and more useful information of how quickly it can be metabolized or excreted by enzymatically or nonenzymatically. To track the drug accumulation and distribution in organism from in vivo PK study, the mass spectrometry imaging and quantification can come up with innovative solutions to quantify dynamic drug exposures in all targeted tissues, or using artificial intelligence modeling to predict the drug exposure in disease or normal organs.   

 

Representaive Case Study from PKMS Core: https://pharmacy.umich.edu/pkcore/supported-work

1. Borkin D, He SH, Miao HZ, Kempinska K, Pollock J, Chase J, Purohit T, Malik B, Zhao T, Wang JY, Wen B, Zong HL, Jones M, Danet-Desnoyers G, Guzman ML, Talpaz M, Bixby DL, Sun DX, Hess JL, Muntean AG, Maillard I, Cierpicki T, Grembecka J. Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo. Cancer Cell. 2015;27(4):589-602. PMCID: PMC4415852

2. Li W, Tanikawa T, Kryczek I, Xia H, Li G, Wu K, Wei S, Zhao L, Vatan L, Wen B, Shu P, Sun D, Kleer C, Wicha M, Sabel M, Tao K, Wang G, Zou W. Aerobic Glycolysis Controls Myeloid-Derived Suppressor Cells and Tumor Immunity via a Specific CEBPB Isoform in Triple-Negative Breast Cancer. Cell Metab. 2018 Jul 3;28(1):87-103.e6. doi: 10.1016/j.cmet.2018.04.022. Epub 2018 May 24. PubMed PMID: 29805099.

3. Kahl, D.J., Hutchings, K.M., Lisabeth, E.M., Haak, A.J., Leipprandt, J.R., Dexheimer, T., Khanna, D., Tsou, P.S., Campbell, P.L., Fox, D.A., Wen, B., Sun, D., Bailie, M., Neubig, R.R. & Larsen, S.D. 5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma. J Med Chem 62, 4350-4369 (2019) PMC6590913.

4. Madak, J.T., Cuthbertson, C.R., Miyata, Y., Tamura, S., Petrunak, E.M., Stuckey, J.A., Han, Y., He, M., Sun, D., Showalter, H.D. & Neamati, N. Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase. J Med Chem 61, 5162-5186 (2018)

5. Zhao Y, Bai L, Liu L, McEachern D, Stuckety JA, Meagher JL, Yang CY, Ran X, Zhou B, Hu Y, Li X, Wen B, Zhao T, Li S, Sun D, Wang S. Structure-based discovery of 4-(6-methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a potent and orally bioavailable BET bromodomain inhibitor. J Med Chem. 2017 May 11;60(9):3887-3901. PMID: 28463487

6Zhao Y, Liu L, Sun W, Lu J, McEachern D, Li X, Yu S, Bernard D, Ochsenbein P, Ferey V, Carry JC, Deschamps JR, Sun D, Wang S. Diastereomeric spirooxindoles as highly potent and efficacious MDM2 inhibitors. J Am Chem Soc. 2013;135(19):7223-34. PMCID: PMC3806051

 

 

Instruments application notes from different company to describe the capability of the each instrument. (UM PKMS core own those cutting-edge technology and instrument to perform similar studies.) 

  1. SCIEX Triple Quad 5500 LC-MS/MS --- Highly Sensitive and Robust Quantification Method for Ethinyl Estradiol and Drospirenone in plasma    https://sciex.com/Documents/tech%20notes/Highly_Sensitive_and_Robust_Quantification.pdf
  2. SCIEX Triple Quad 5500 Qtrap system --- In Vivo Metabolic Profiling of Carbamazepine Using the QTRAP® 5500 System and LightSight® Software v2.2   https://sciex.com/Documents/Downloads/Literature/mass-spectrometry-Carbamazepine-profiling-1036610.pdf
  3. SCIEX X500R QTOF system --- Using MS/MSall with SWATH Acquisition For Forensic Designer Drug Analysis with SCIEX X500R QTOF system and SCIEX OS Software https://sciex.com/Documents/tech%20notes/forensic-designer-drug-analysis.pdf
  4. SCIEX X500R QTOF system --- Rapid Metabolite Identification using MetabolitePilot™ Software and TripleTOF™ 5600 system   https://sciex.com/Documents/Downloads/Literature/Rapid_Metabolite_Identification_using_MetabolitePilot_Software.pdf
  5. SYNAPT G2-Si HDMS QTOF system --- Targeted High Resolution Quantification with Tof-MRM and HD-MRM http://www.waters.com/webassets/cms/library/docs/720004728EN.pdf 
  6. Waters SYNAPT G2-Si HDMS QTOF system --- Qualitative and Quantitative Metabolite Identification for Verapamil in Rat Plasma Using a UPLC/SYNAPT G2 HDMS Strategy with MSE   http://www.waters.com/webassets/cms/library/docs/720003492en.pdf
  7.  Waters SYNAPT G2-Si HDMS QTOF system --- Ion Mobility Separation Coupled With Desorption Electrospray Ionization Mass Spectrometry for High Specificity MS Imaging   http://www.waters.com/webassets/cms/library/docs/720005525en.pdf
  8. Waters SYNAPT G2-Si HDMS QTOF system --- Lipid Visualization and Identification Through Collisional Cross Section Aided Correlation of MS Imaging and Ex Situ MS Data for MS-MS Identification   http://www.waters.com/webassets/cms/library/docs/720005354en.pdf

Edited by Bo Wen, 05/2020 

Mass spectrometry imaging (MSI)  is an emerging technique that allows molecular visualization of the distribution of drugs, lipids, peptides, proteins and metabolites in a two-dimensional space directly in biological tissues. MSI allows unlabeled drug compounds and drug metabolites to be detected and identified and quantified according to their mass-to-charge ratios (m/z) at high resolution in complex tissue environments. This technique has better specificity and provides the possibility to combine histological data with MS ones and to visualize simultaneously the distribution drugs or biomarkers in relation to tumor heterogeneity, provide new understandings of the dynamic processes impacting drug uptake and metabolism at the local sites targeted by therapy.

 

We have a state of the art MALDI/DESI SYNAPT G2-Si High Definition Mass Spectrometry (Waters®) in our Pharmacokinetics and Mass Spectrometry Core Facility (PKMS). Using the MALDI and DESI ion source together with T-Wave ion mobility technology, our experienced team of mass spectrometry imagers can provide distribution profiling information for a wide range of sample types, such as tissue specimens, industrial and biological materials, horticultural specimens, and microbiological populations. We offer MSI sample preparation, including cryo-sectioning and microtome techniques, histological staining, and tissue microscopy. We can also combine imaging data with data acquired by different analytical techniques to deliver more comprehensive results. Our team works with you to identify MSI approaches to address your application requirements.

  • Drug development
  • Pharmacokinetics: Drug and Metabolite Distribution, 2D and 3D label free Imaging
  • Disease characterization and biomarker investigations
  • Carcinomas
  • Inter-and intra-tumor heterogeneity
  • Inflammatory diseases
  • Fibrosis
  • Bacterial infections and manifestations
  • Neurological diseases
PKMS Case study 1 : small molecular or lipids mass spectrometry imaging on mouse brain tissue section, thousand compounds can be imaged from the same tissue section at same time. 

          M/Z  253.08                            M/Z  314.11                           M/Z  495.02                            M/Z  831.45                                                                                                                                                 

PKMS Case study 2 : MALDI-Ion mobility mass spectrometry imaging for paclitaxel ditribution in solid tumor tissue.   https://pharmacy.umich.edu/pkcore/Conference%20Poster

 

Instruments application notes from Waters® to describe the capability of the SYNAPT G2-Si High Definition Mass Spectrometry.

  1. Biomarker Discovery Directly from Tissue Xenograph Using High Definition Imaging MALDI Combined with Multivariate Analysis. http://www.waters.com/webassets/cms/library/docs/720004873en.pdf
  2. Data Independent MALDI Imaging HDMSE for Visualization and Identification of Lipids Directly from a Single Tissue Section. http://www.waters.com/webassets/cms/library/docs/720004471en.pdf
  3. Distribution of Biomarkers of Interest in Rat Brain Tissues Using High Definition MALDI Imaging. http://www.waters.com/webassets/cms/library/docs/720004135en.pdf
  4. MALDI Imaging of Distribution of Xanthohumol and Its Metabolites in Rat Tissues. http://www.waters.com/webassets/cms/library/docs/720003707en.pdf
  5. Successful Application for Distribution Imaging of Chloroquine Ocular Tissue in Pigmented Rat Using MALDI-Imaging Quadrupole Time-of-Flight Mass Spectrometry. http://www.waters.com/waters/library.htm?locale=en_SE&cid=10010845&lid=10180348
  6. MALDI-Ion Mobility Separation-Mass Spectrometry Imaging of Glucose-Regulated Protein 78 kDa (Grp78) in Human Formalin-Fixed, Paraffin-Embedded Pancreatic Adenocarcinoma Tissue Sections. https://pubs.acs.org/doi/abs/10.1021/pr900522m
  7. Tissue Imaging of Pharmaceuticals by Ion Mobility Mass Spectrometry. http://www.waters.com/webassets/cms/library/docs/720003216en.pdf
  8. Direct Tissue Imaging and Characterization of Phospholipids Using MALDI SYNAPT HDMS System. http://www.waters.com/webassets/cms/library/docs/720002444en.pdf
  9. Localizing Diazepam and its Metabolite in Rat Brain Tissue by Imaging Mass Spectrometry using MALDI Q-Tof Premier MS. http://www.waters.com/webassets/cms/library/docs/720002447en.pdf
  10. Matrix-Assisted Laser Desorption/Ionization-Ion Mobility Separation-Mass Spectrometry Imaging of Vinblastine in Whole Body Tissue Sections. https://pubs.acs.org/doi/abs/10.1021/ac8015467

Edited by Bo Wen, 05/2020  

The use of bioanalytical technologies such as quantitative liquid chromatography-mass spectrometry (LC-MS/MS) has been accepted as the gold-standard technology to support PK and drug metabolism studies. It comes significant improvements in assay sensitivity, selective and specificity, plus the potential to reduce assay time per samples, and the detection of compounds of interest in different matrices, no matter how complex - including plasma, blood, serum, urine, faces, spinal fluid, skin, muscle, artery, myocardium, liver and kidney, and a variety of tumor types. Below is list of drug that have been tested in our core with an validated LC-MS assay.  

 

Compound Name  Classification Transition Ions ( M/Z) Limit of Detection
Acalabrutinib Bruton's tyrosine kinase inhibitor 466.0→372.3 0.2 ng/mL in rat plasma 
Adenosine Nucleoside 268.0→136.0 5 ng/ml in plasma
Afatinib Tyrosine kinase inhibitor 486.1→370.9 0.5 ng/mL in human plasma
Amifostine Chemoprotective agent HRMS HRMS
Aminocaproic Acid Clotting promoter 132.1→95.9 10 ng/mL in human plasma
Amlexanox Anti-inflammatory agent 297.1→253.2  1 ng/mL in mice serum 
Apcin Cell cycle inhibitor  438.1→224.0 2 ng/mL in mice plasma
Apixaban Anticoagulant 460.2→443.2 1 ng/mL in human plasma 
Arachidonoyl Glycine Lipids 362.5→278.0 1 ng/mL in acetonitrile
Aripiprazole Atypical antipsychotic 448.2→285.2 1 ng/mL in plasma or brain
Artemether Antimalarial 316.2→267.2 2 ng/mL in human plasma 
Azithromycin Antibiotic  479.5→591.4 1 ng/mL in rat blood or brain
Buprenorphine Narcotic 468.1→396.2 0.1 ng/mL in mice plasma
Bupropion Antidepressant 240.0→184.0 0.5 ng/mL in human plasma
Carprofen Nonsteroidal anti-inflammatory drug 272.0→228.1 5 ng/mL in mouse plasma
Cefaclor Second-generation cephalosporin antibiotic 368.0→174.0 2 ng/mL in human plasma 
Cefazolin Antibiotic 455.2→323.0 10 ng/mL in human plasma 
Chlorambucil Chemotherapy 303.9→192.0 50 ng/mL in mouse plasma
Cholesterol Sterol 369.3→369.3 10 ng/mL in solution
Cisplatin Chemotherapy 492.0→426.0 1 ng/ml in urine
Clofazimine substituted iminophenazine dye 473.0→431.1 1 ng/ml in mouse serum
Concanamycin A plecomacrolide antibiotic 888.8→515.2 0.1 ng/mL in mouse plasma
Cyclophosphamide Chemotherapy 261.0→140.0 1 ng/mL in human plasma 
Dabrafenib Kinase inhibitors 520.0→343.1 1 ng/ml in mouse plasma 
Dacomitinib multi-kinase receptor inhibitor 470.0→385.0  1 ng/mL in rat plasma 
Daptomycin Antibiotic 811.3→ 341.4 1 ng/mL in feces
Dasatinib Chemotherapy 488.3→ 401.2 1 ng/mL in plasma
Deoxyuridine Antiviral 237.1→137.0 5 ng/ml in plasma
Dexamethasone Corticosteroid 393.0→373.0 2.5 ng/mL  in plasma
Docetaxel Chemotherapy 808.4→225.9 1 ng/mL in plasma
Doxorubicin Chemotherapy 544.0→361.0 2 ng/mL in plasma
Doxycycline Antibiotic 445.2→ 321.0 2.5 ng/mL in plasma
Echinomycin Antibiotic 1101.1→1053.2 0.1 ng/mL in plasma
Eliglustat Gastrointestinal system drug 405.1→316.2 1 ng/mL in plasma
Entrectinib Chemotherapy 561.0→302.1   1 ng/mL in plasma
Ertapenem Antibiotic 476.1→346.1 100 ng/mL in plasma
Etonogestrel Contraceptive drug 325.2→257.2 0.25 ng/mL in plasma
Everolimus Immunosuppressive agent 980.2→389.1  1 ng/mL in plasma
Fedratinib Inhibitor of myelfobrosis 525.1→525.1 1 ng/mL in plasma
Fentanyl Narcotic 337.2→188.2  1 ng/mL in plasma
Ferioxamine Supply of iron 614.4→414.4 0.48 nM in water
Fingolimod Immunosuppressive drug 308.4→255.1 1 ng/mL in plasma
Floxuridine Chemotherapy 245.1→155.0 2 ng/mL in liver sample
Fluticasone Antiallergy medicine 501.0→293.2 3 ng/mL in plasma
Fluticasone Propionate Steroid and Decongestant 501.2→293.2 1 ng/mL in plasma
Fulvestrant Chemotherapy 605.2→427.4 0.1 ng/mL in plasma
Gallein Chemotherapy 365.1→189.0 5 ng/mL in plasma
Glucoraphanin Supplement 438.0→196.0 2 ng/mL in urine
Ibrutinib Chemotherapy 441.1→138.1 1 ng/mL in plasma
Ibuprofen Nonsteroidal anti-Inflammatory drug 205.1→125.0 5 ng/mL in plasma
Imatinib Chemotherapy 372.5 → 176.3 0.5 ng/mL in plasma
Larotrectinib Chemotherapy 429.0 → 342.0 1 ng/mL in plasma
Leuprolide Hormones 605.5 → 221 0.1 ng/mL in plasma
Mesalamine Nonsteroidal anti-Inflammatory drug 152.0 → 108.0 1 ng/mL in plasma
Metformin Diabetes medication 130.1 → 71.1 5 ng/mL in plasma
Metoprolol Beta blocker 268.2→116.2 1 ng/mL in human serum
metronidazole Antibiotic 172.1→128 10 ng/mL in tissue
Mianserin Antidepressant 266.0→209.0 1 ng/mL in plasma
Nalbuphine Narcotic 358.2→340.2  0.5 ng/mL in mouse plasma
Naloxone Narcotic 327.6→309.6 0.5 ng/mL in monkey plasma
Neratinib Chemotherapy 557.1→512.0 1 ng/mL in plasma
Nilotinib Chemotherapy 530.1→307.2 1 ng/mL in mouse plasma
Olaparib Chemotherapy 435.3→281.2 1 ng/mL in mouse plasma
Osimertinib Chemotherapy 500.2→71.8 1 ng/mL in plasma
oxalate nature compound HRMS 1 ug/mL in plasma
Paclitaxel Chemotherapy 854.4→286.1 1 ng/mL in human plasma
Panobinostat Chemotherapy 350.2→158.1 1 ng/mL in mouse plasma
Paroxetine Antidepressant 330.1→192.2 1 ng/mL in mouse plasma
Pazopanib Chemotherapy 438.1→357.2 1 ng/mL in human  plasma
Pemetrexed Chemotherapy 428.3→281.1 25 pg/mL in urine
Piperacillin Antibiotic 518.0→359.0 5 ng/mL in plasma
Pomalidomide  Immunomodulatory drug 274.02→201.00 0.1 ng/mL in mouse plasma
Ponatinib Chemotherapy  533.3→231.9 1 ng/mL in mouse plasma and brain 
Propranolol Hydrochloride Beta-blocker 260.3→260.3 5 nM for dissolution studies
Rafarm Iron supplement Chelatable iron is detected by HPLC-UV 15.6 µM in saline and rat serum
Selumetinib Chemotherapy  459.0→301.1 10 ng/mL in rat plasma
Simvastatin Antilipemic agent  436.3→285.2 0.1 ng/mL in mouse plasma and liver 
Sirolimus Immunosuppressive drug 931.5→864.6 0.5 ng/mL in human blood
Solifenacin Bladder relaxant 363→193 0.5 ng/mL in human plasma
sorafenib Chemotherapy 465→252 10 ng/mL in human plasma
Sulfadiazine Antibiotic 251.1→156.0 400 µM for dissolution studies
Sulforaphane Supplement 178 → 113.6 1 ng/mL in rat plasma
Tacrolimus Immunosuppressive drug 821.4→768.5 0.5 ng/mL in human blood
Tamiflu Antiviral drug 313.2→166.1 0.5 ng/mL in human plasma
Tamoxifen Chemotherapy 372.1→72.0 1 ng/mL in mouse plasma and tissues 
Tazobactam Antibiotic 299.0→138/254.9 0.25 µg/mL in human plasma
Thymoquinone Chemotherapy HPLC-UV  
Tofacitinib Antineoplastic  313.1→173.1 1 ng/mL in mouse plasma
Trametinib Chemotherapy 616→491.0 1 ng/mL in mouse plasma
Triamcinolone Acetonide Steroid 435→415 10.0 pg/mL in rabit plasma
Valproic Acid Anticonvulsant 143.0→143.0  5 µg/mL in human plasma
Vancomycin Antibiotic 725.6 → 100.2  0.05 ng/mL in human plasma
Varenicline Smoking Cessation Agent 212.1 → 169.1 0.1 ng/mL in human plasma
Vemurafenib Chemotherapy 490.1→383.1 100 ng/mL in mouse plasma
Venofer  Iron supplement Chelatable iron is detected by HPLC-UV 15.6 µM in saline and rat serum
Withaferin A Supplement 471.1→281 2 ng/mL in rat plasma and tissues
Zanamivir Antiviral drug 333→60 1 ng/mL in human plasma

Edited by Bo Wen, 06/09/20  

Pharmacokinetics

Pharmacokinetics (PK) is the study of the time course of drug’s absorption, distribution, metabolism, and excretion (ADME), what the body interact with a drug, related to the movement of drug into, pass, and out of the body. In order for a drug to be effective in the body, enough of the active form must reach the target to elicit the desired effect. The compound with the best activity against the target enzyme or receptor may have very poor ADME characteristics such as metabolic instability or poor intestinal absorption. When choosing a lead candidate from multiple compounds, the activity of the drug in the efficacy screen must be balanced with acceptable ADME and stability characteristics. Pharmacokinetic studies with mass spectrometry bioanalysis can provide the quantitative information about the half-life of the administrated compound from in vitro and in vivo test, and more useful information of how quickly it can be metabolized or excreted by enzymatically or nonenzymatically. To track the drug accumulation and distribution in organism from in vivo PK study, the mass spectrometry imaging and quantification can come up with innovative solutions to quantify dynamic drug exposures in all targeted tissues, or using artificial intelligence modeling to predict the drug exposure in disease or normal organs.   

Capture PK.JPG

A typical plot of plasma concentration versus time following the oral administration
Mass Spec Imaging

Mass spectrometry imaging (MSI)  is an emerging technique that allows molecular visualization of the distribution of drugs, lipids, peptides, proteins and metabolites in a two-dimensional space directly in biological tissues. MSI allows unlabeled drug compounds and drug metabolites to be detected and identified and quantified according to their mass-to-charge ratios (m/z) at high resolution in complex tissue environments. This technique has better specificity and provides the possibility to combine histological data with MS ones and to visualize simultaneously the distribution drugs or biomarkers in relation to tumor heterogeneity, provide new understandings of the dynamic processes impacting drug uptake and metabolism at the local sites targeted by therapy.

UM PKMS MSI Workflow.png

UM PKMS MSI Workflow
LCMS Bioanalytical Assays

The use of bioanalytical technologies such as quantitative liquid chromatography-mass spectrometry (LC-MS/MS) has been accepted as the gold-standard technology to support PK and drug metabolism studies. It comes significant improvements in assay sensitivity, selective and specificity, plus the potential to reduce assay time per samples, and the detection of compounds of interest in different matrices, no matter how complex - including plasma, blood, serum, urine, faces, spinal fluid, skin, muscle, artery, myocardium, liver and kidney, and a variety of tumor types. Below is list of drug that have been tested in our core with an validated LC-MS assay.  

 

Compound Name  Classification Transition Ions ( M/Z) Limit of Detection
Acalabrutinib Bruton's tyrosine kinase inhibitor 466.0→372.3 0.2 ng/mL in rat plasma 
Adenosine Nucleoside 268.0→136.0 5 ng/ml in plasma
Afatinib Tyrosine kinase inhibitor 486.1→370.9 0.5 ng/mL in human plasma
Amifostine Chemoprotective agent HRMS HRMS
Aminocaproic Acid Clotting promoter 132.1→95.9 10 ng/mL in human plasma
Amlexanox Anti-inflammatory agent 297.1→253.2  1 ng/mL in mice serum 
Apcin Cell cycle inhibitor  438.1→224.0 2 ng/mL in mice plasma
Apixaban Anticoagulant 460.2→443.2 1 ng/mL in human plasma 
Arachidonoyl Glycine Lipids 362.5→278.0 1 ng/mL in acetonitrile
Aripiprazole Atypical antipsychotic 448.2→285.2 1 ng/mL in plasma or brain
Artemether Antimalarial 316.2→267.2 2 ng/mL in human plasma 
Azithromycin Antibiotic  479.5→591.4 1 ng/mL in rat blood or brain
Buprenorphine Narcotic 468.1→396.2 0.1 ng/mL in mice plasma
Bupropion Antidepressant 240.0→184.0 0.5 ng/mL in human plasma
Carprofen Nonsteroidal anti-inflammatory drug 272.0→228.1 5 ng/mL in mouse plasma
Cefaclor Second-generation cephalosporin antibiotic 368.0→174.0 2 ng/mL in human plasma 
Cefazolin Antibiotic 455.2→323.0 10 ng/mL in human plasma 
Chlorambucil Chemotherapy 303.9→192.0 50 ng/mL in mouse plasma
Cholesterol Sterol 369.3→369.3 10 ng/mL in solution
Cisplatin Chemotherapy 492.0→426.0 1 ng/ml in urine
Clofazimine substituted iminophenazine dye 473.0→431.1 1 ng/ml in mouse serum
Concanamycin A plecomacrolide antibiotic 888.8→515.2 0.1 ng/mL in mouse plasma
Cyclophosphamide Chemotherapy 261.0→140.0 1 ng/mL in human plasma 
Dabrafenib Kinase inhibitors 520.0→343.1 1 ng/ml in mouse plasma 
Dacomitinib multi-kinase receptor inhibitor 470.0→385.0  1 ng/mL in rat plasma 
Daptomycin Antibiotic 811.3→ 341.4 1 ng/mL in feces
Dasatinib Chemotherapy 488.3→ 401.2 1 ng/mL in plasma
Deoxyuridine Antiviral 237.1→137.0 5 ng/ml in plasma
Dexamethasone Corticosteroid 393.0→373.0 2.5 ng/mL  in plasma
Docetaxel Chemotherapy 808.4→225.9 1 ng/mL in plasma
Doxorubicin Chemotherapy 544.0→361.0 2 ng/mL in plasma
Doxycycline Antibiotic 445.2→ 321.0 2.5 ng/mL in plasma
Echinomycin Antibiotic 1101.1→1053.2 0.1 ng/mL in plasma
Eliglustat Gastrointestinal system drug 405.1→316.2 1 ng/mL in plasma
Entrectinib Chemotherapy 561.0→302.1   1 ng/mL in plasma
Ertapenem Antibiotic 476.1→346.1 100 ng/mL in plasma
Etonogestrel Contraceptive drug 325.2→257.2 0.25 ng/mL in plasma
Everolimus Immunosuppressive agent 980.2→389.1  1 ng/mL in plasma
Fedratinib Inhibitor of myelfobrosis 525.1→525.1 1 ng/mL in plasma
Fentanyl Narcotic 337.2→188.2  1 ng/mL in plasma
Ferioxamine Supply of iron 614.4→414.4 0.48 nM in water
Fingolimod Immunosuppressive drug 308.4→255.1 1 ng/mL in plasma
Floxuridine Chemotherapy 245.1→155.0 2 ng/mL in liver sample
Fluticasone Antiallergy medicine 501.0→293.2 3 ng/mL in plasma
Fluticasone Propionate Steroid and Decongestant 501.2→293.2 1 ng/mL in plasma
Fulvestrant Chemotherapy 605.2→427.4 0.1 ng/mL in plasma
Gallein Chemotherapy 365.1→189.0 5 ng/mL in plasma
Glucoraphanin Supplement 438.0→196.0 2 ng/mL in urine
Ibrutinib Chemotherapy 441.1→138.1 1 ng/mL in plasma
Ibuprofen Nonsteroidal anti-Inflammatory drug 205.1→125.0 5 ng/mL in plasma
Imatinib Chemotherapy 372.5 → 176.3 0.5 ng/mL in plasma
Larotrectinib Chemotherapy 429.0 → 342.0 1 ng/mL in plasma
Leuprolide Hormones 605.5 → 221 0.1 ng/mL in plasma
Mesalamine Nonsteroidal anti-Inflammatory drug 152.0 → 108.0 1 ng/mL in plasma
Metformin Diabetes medication 130.1 → 71.1 5 ng/mL in plasma
Metoprolol Beta blocker 268.2→116.2 1 ng/mL in human serum
metronidazole Antibiotic 172.1→128 10 ng/mL in tissue
Mianserin Antidepressant 266.0→209.0 1 ng/mL in plasma
Nalbuphine Narcotic 358.2→340.2  0.5 ng/mL in mouse plasma
Naloxone Narcotic 327.6→309.6 0.5 ng/mL in monkey plasma
Neratinib Chemotherapy 557.1→512.0 1 ng/mL in plasma
Nilotinib Chemotherapy 530.1→307.2 1 ng/mL in mouse plasma
Olaparib Chemotherapy 435.3→281.2 1 ng/mL in mouse plasma
Osimertinib Chemotherapy 500.2→71.8 1 ng/mL in plasma
oxalate nature compound HRMS 1 ug/mL in plasma
Paclitaxel Chemotherapy 854.4→286.1 1 ng/mL in human plasma
Panobinostat Chemotherapy 350.2→158.1 1 ng/mL in mouse plasma
Paroxetine Antidepressant 330.1→192.2 1 ng/mL in mouse plasma
Pazopanib Chemotherapy 438.1→357.2 1 ng/mL in human  plasma
Pemetrexed Chemotherapy 428.3→281.1 25 pg/mL in urine
Piperacillin Antibiotic 518.0→359.0 5 ng/mL in plasma
Pomalidomide  Immunomodulatory drug 274.02→201.00 0.1 ng/mL in mouse plasma
Ponatinib Chemotherapy  533.3→231.9 1 ng/mL in mouse plasma and brain 
Propranolol Hydrochloride Beta-blocker 260.3→260.3 5 nM for dissolution studies
Rafarm Iron supplement Chelatable iron is detected by HPLC-UV 15.6 µM in saline and rat serum
Selumetinib Chemotherapy  459.0→301.1 10 ng/mL in rat plasma
Simvastatin Antilipemic agent  436.3→285.2 0.1 ng/mL in mouse plasma and liver 
Sirolimus Immunosuppressive drug 931.5→864.6 0.5 ng/mL in human blood
Solifenacin Bladder relaxant 363→193 0.5 ng/mL in human plasma
sorafenib Chemotherapy 465→252 10 ng/mL in human plasma
Sulfadiazine Antibiotic 251.1→156.0 400 µM for dissolution studies
Sulforaphane Supplement 178 → 113.6 1 ng/mL in rat plasma
Tacrolimus Immunosuppressive drug 821.4→768.5 0.5 ng/mL in human blood
Tamiflu Antiviral drug 313.2→166.1 0.5 ng/mL in human plasma
Tamoxifen Chemotherapy 372.1→72.0 1 ng/mL in mouse plasma and tissues 
Tazobactam Antibiotic 299.0→138/254.9 0.25 µg/mL in human plasma
Thymoquinone Chemotherapy HPLC-UV  
Tofacitinib Antineoplastic  313.1→173.1 1 ng/mL in mouse plasma
Trametinib Chemotherapy 616→491.0 1 ng/mL in mouse plasma
Triamcinolone Acetonide Steroid 435→415 10.0 pg/mL in rabit plasma
Valproic Acid Anticonvulsant 143.0→143.0  5 µg/mL in human plasma
Vancomycin Antibiotic 725.6 → 100.2  0.05 ng/mL in human plasma
Varenicline Smoking Cessation Agent 212.1 → 169.1 0.1 ng/mL in human plasma
Vemurafenib Chemotherapy 490.1→383.1 100 ng/mL in mouse plasma
Venofer  Iron supplement Chelatable iron is detected by HPLC-UV 15.6 µM in saline and rat serum
Withaferin A Supplement 471.1→281 2 ng/mL in rat plasma and tissues
Zanamivir Antiviral drug 333→60 1 ng/mL in human plasma

Edited by Bo Wen, 06/09/20  

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Tuesday, May 10, 2016
Tuesday, May 10, 2016