Lesson plan

Dactolisib

Dactolisib (codenamed NVP-BEZ235 and BEZ-235, also known as RTB101) is an imidazoquinoline derivative acting as a PI3K inhibitor. It also inhibits mTOR. It is being investigated as a possible cancer treatment. It has been shown to be toxic to Waldenström's macroglobulinemia cells. It was the first PI3K inhibitor to enter clinical trials, in 2006. A phase IB/II clinical trial for locally advanced or metastatic HER2 negative breast cancer has completed. A phase II clinical trial for advanced pancreatic neuroendocrine tumors (pNET) had initially reported results, but was later terminated because insufficient normal tissue tolerance to the drug. A phase I clinical trial of BEZ235 in patients with advanced renal cell carcinoma had to be terminated prematurely due to toxicity and a lack of clinical efficacy . Another Phase Ib study on patients with various solid cancers found severe normal tissue toxicity as well when BEZ235/Dactolisib was administered in combination with the mTOR inhibitor Everolimus. The authors concluded that the combination of both drugs demonstrated limited efficacy and tolerance. BEZ235 systemic exposure increased in a dose-proportional manner while oral bioavailability was quite low, which may be related to gastrointestinal-specific toxicity .…

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Article summary

Dactolisib (codenamed NVP-BEZ235 and BEZ-235, also known as RTB101) is an imidazoquinoline derivative acting as a PI3K inhibitor. It also inhibits mTOR. It is being investigated as a possible cancer treatment. It has been shown to be toxic to Waldenström's macroglobulinemia cells. It was the first PI3K inhibitor to enter clinical trials, in 2006. A phase IB/II clinical trial for locally advanced or metastatic HER2 negative breast cancer has completed. A phase II clinical trial for advanced pancreatic neuroendocrine tumors (pNET) had initially reported results, but was later terminated because insufficient normal tissue tolerance to the drug. A phase I clinical trial of BEZ235 in patients with advanced renal cell carcinoma had to be terminated prematurely due to toxicity and a lack of clinical efficacy . Another Phase Ib study on patients with various solid cancers found severe normal tissue toxicity as well when BEZ235/Dactolisib was administered in combination with the mTOR inhibitor Everolimus. The authors concluded that the combination of both drugs demonstrated limited efficacy and tolerance. BEZ235 systemic exposure increased in a dose-proportional manner while oral bioavailability was quite low, which may be related to gastrointestinal-specific toxicity .…

Key claims

  1. publication date: 2018 — source: Wikipedia · confidence 0.95

Discussion questions

  1. Summarise the article in your own words. Which single claim would you verify first, and why?
  2. The record states that the publication date is "2018". What evidence would count against this claim?
  3. Which claim in this article is most likely to be revised as the sources update? How would you check its current status?
  4. If two sources disagreed about one of these facts, what would you need in order to trust one over the other?

Bibliography

  1. Wikipedia https://en.wikipedia.org/w/index.php?oldid=1330099753

Key claims and bibliography are generated from the same tracked claims and sources as the article page.