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The main metabolites in humans biologically active

Max 3-4 pages, do not skip each question, each bullet !!


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Please obtain from the web the 2010 paper by Nomura et al. on the discovery of canagliflozin.

· The title is: “Discovery of Canagliflozin, a Novel C-Glucoside with Thiophene Ring, as Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes Mellitus”.

· Also download the Supplemental Information

You may need to get additional information from Google, Wikipedia, or PubMed

Prepare a short summary of the properties of canagliflozin:

· Compound number on the paper, MW, and structure

· Originator and marketing companies (Wiki)

· Explain (one bullet) how the in vitro assays at SGLT-1 and SGLT-2 were performed

· Potency and selectivity at the relevant transporters in vitro

· Relevant PK parameters

· Pharmacodynamic effects in mice (do not forget to indicate doses and route of administration)

· Explain why the authors used “KK mice” (one bullet)

· Summary evaluation of the compound and its status in 2010

Please retrieve the 2014 paper by Mamidi et al. on the metabolism of canagliflozin.

· Provided

Prepare a short summary:

· Title, authors, company, and citation (can copy/paste from pdf)

· Proposed in vivo metabolic pathways for canagliflozin in mice, rats, dogs, and humans

· Indicate on the above scheme the metabolites find in humans

· Add to the above scheme the CYPs and UGTs responsible for each metabolite found in humans (Hint: read the Discussion)

· Graph of PK of canagliflozin and metabolites in humans

· Which is the primary biotransformation pathway of canagliflozin in humans?

· What are the main differences in metabolism and excretion between animals and humans?

· Are the main metabolites in humans biologically active?

· Why wasn’t it necessary to test the non-clinical safety of the main human metabolites?

Please retrieve the 2013 paper by F. J. Lavalle-González et al. on a clinical trial with canagliflozin in T2D

· Provided

Prepare and describing details and results of the trial as suggested below.

This should be very easy for the students by now!

· Copy/paste the title portion of the paper with title, authors, citation, and also the addresses of all the authors

· We want to know who they are and where they work

· Go to and find the trial using its NCT number. Navigate to the “Tabular View” tab, which is easier to read. On your slide provide the following information (Try to copy/paste as much as possible):

· NCT number

· Brief Title

· Official Title

· Responsible Party

· Study Sponsor

· Study Director

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