Tag: non-small cell lung cancer (nsclc)

Pharmacology Digest, July 29th, 2018

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Erlotinib (Tarceva®)

Erlotinib is an epidermal growth factor receptor (EGFR) used in the treatment of advanced pancreatic cancer and some types of lung cancer.  It interacts with the intracellular ATP-binding site of the tyrosine kinase of EGFR, inhibiting downstream RAS, PI3K and STAT signaling pathways.  Erlotinib produces cell cycle blockade, slowed angiogenesis and decreased tumor burden in responsive malignancies.

Erlotinib is specifically indicated for unresectable or metastatic pancreatic cancer and non-small cell lung cancer (NSCLC) with exon 19 deletion or an L to R mutation at site 858.  Its efficacy in lung cancer with other EGFR mutations has not yet been established.

Erlotinib therapy may cause significant toxicity, with around 1% of patients developing interstitial lung disease.  Some patients have also experienced hepatotoxicity, GI perforation, severe skin disorders, and ocular dysfunction.  The most common side effects are nausea, diarrhea, rash, and fatigue.

 

erlotinib

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 May 7.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRxhttp://www.goodrx.com
  4. “DailyMed.” U.S. National Library of Medicine, National Institutes of Health, dailymed.nlm.nih.gov/dailymed/.

 

Checkpoint Inhibitor Combo > Chemo in Some Lung Cancers | NEJM

Non-small cell lung cancer (NSCLC) patients with high tumor mutational burden (>10 mutations/megabase) were selected for a phase III clinical trial comparing combination checkpoint inhibitor therapy to platinum-based chemotherapy.

A combination regimen of Nivolumab, an anti–programmed death 1 (PD-1) antibody, and ipilimumab, an anti–cytotoxic T-lymphocyte antigen 4 (CTLA-4) antibody resulted in significantly better 1-year survival (42%) than platinum-doublet chemotherapy (13%).

 

 

Original Article from The New England Journal of Medicine — Nivolumab plus Ipilimumab in Lung Cancer with a High Tumor Mutational Burden

Source: Nivolumab plus Ipilimumab in Lung Cancer with a High Tumor Mutational Burden | NEJM

Paclitaxel (Taxol®, Abraxane®) – Taxane Antineoplastic

Paclitaxel is a taxane-class cytotoxic chemotherapeutic agent for cancer treatment.

Paclitaxel inhibits microtubule depolymerization in dividing cells, blocking the metaphase-anaphase transition and eventually leading to apoptosis.  Lack of specificity for tissue type have made this drug a mainstay of treatment for a variety of malignancies, especially those of the ovary, breast, and lung, while also underlying its significant off-target toxicity.

Patients should be pre-treated with corticosteroids and anti-histamines due to a relatively high risk of severe hypersensitivity reactions during infusion.

paclitaxel

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 April 25.