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Homework answers / question archive / 1)RETEVMO selpercatinib (short answer 2-3 pages) Obtain the label (prescribing information) of selpercatinib in pdf form from the web

1)RETEVMO selpercatinib (short answer 2-3 pages) Obtain the label (prescribing information) of selpercatinib in pdf form from the web

Biology

1)RETEVMO selpercatinib (short answer 2-3 pages)

Obtain the label (prescribing information) of selpercatinib in pdf form from the web. If necessary, always say that you are a US healthcare provider, which is the truth. The purpose of this presentation request is to familiarize you with reading labels from the point of view of a Pharma scientist.

summarizing specific characteristics of the drug as listed below:

· Commercial name, international nonproprietary name (INN), structure, molecular weight, and sponsor company name

· Show the three indications of selpercatinib (omit less essential details)

· What is the general pharmacological action of the drug?

· What is the intended molecular target*?

· List all the other kinases it inhibits.

· In what form is the drug provided?

· What is the dose and frequency of administration? (For body weight > 50 kg)

· How does selpercatinib affect QTc interval in healthy subjects (Section 12.2)? What should the physician do with patients at risk of developing QTc prolongation (few words)?

· What are the bioavailability and half-life of selpercatinib?

· What was the Cmax (at 160 mg BID) in ng/ml and nM ? What was the PPB and the concentration of free drug (in nM) at Cmax at this dose?

· Which CYP450 is responsible for most of selpercatinib metabolism?

· What was the effect of coadministration of strong CYP3A inhibitors? (Assume they mean CYP3A4)

· What was the effect of coadministration of Pgp inhibitors?

· Which transporters does selpercatinib inhibit*?

 

 

2: Amgen SAR paper

 

· Please download the paper by Miranda et al. (2008) and summarize

· What type of compounds are the authors trying to obtain and for what clinical indication?

· Design a little PowerPoint table showing for Cpd 1, Cpd 2, the most potent, and the most stable (in plasma in vitro) peptides made by the authors:

· The compound number on the paper (abbreviated: Cpd.)

· Its peptide sequence, showing the amino acids changed relative to Cpd. 1 (bold or in some color)

· Its potency as an antagonist

· How are the N-terminus and the C-terminus of the most stable peptide modified?

· How many unnatural amino acids does the most stable peptide contain (hint: not represented by a capital letter)?

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