Small molecules

• larotrectinib
  8 November 2019

  WKP
  Larotrectinib (tradename Vitrakvi) is an inhibitor of tropomyosin kinase receptors NTRKs TrkA , TrkB , and TrkC. It was discovered by Array BioPharma and licensed to Loxo Oncology in 2013.

• tofacitinib
  14 June 2017

  Xeljanz Jakvinus WKP
  Tofacitinib (INN) is a janus kinase (JAK ) inhibitor class, discovered and developed by the National Institutes of Health and Pfizer. Tofacitinib is marketed as Xeljanz and Jakvinus.
  It is currently approved for the treatment of rheumatoid arthritis (RA) in the United States and other countries.
  It has demonstrated effectiveness in the treatment of psoriasis in Phase 3 studies. It is being studied for treatment of inflammatory bowel disease, and other (...)

• idelalisib
  19 April 2017

  WKP
  Idelalisib (trade name Zydelig, codenamed GS-1101 or CAL-101) is a drug used for the treatment of certain hematological malignancies.
  The substance acts as a phosphoinositide 3-kinase inhibitor / PI-3Ks inhibitor; more specifically, it blocks P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase.
  PI3K(s)) are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in (...)

• entrectinib
  24 January 2017

  RXDX-101, NMS-E628 ; Rozlytrek WKP
  Definition: Entrectinib is an investigational drug with preliminary antitumor activity. It is a selective tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (Trk) A, B and C, C-ros oncogene 1 (ROS1 ) and anaplastic lymphoma kinase (ALK ).
  In the U.S., entrectinib has orphan drug designation and rare pediatric disease designation for the treatment of neuroblastoma and orphan drug designation for treatment of TrkA-, TrkB-, TrkC-, (...)

• abemaciclib
  14 December 2016

  LY2835219
  |WKP|
  Abemaciclib is a CDK inhibitor selective for CDK4 and CDK6.
  It is an investigational drug for various types of cancer developed by Eli Lilly. It was designated as a breakthrough therapy by the U.S. Food and Drug Administration in October 2015.
  See also
  CDK4/6 inhibitors

• osimertinib
  2 November 2016

  WKP
  Osimertinib (previously known as mereletinib or AZD9291; trade name Tagrisso) is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug, developed by AstraZeneca Pharmaceuticals – for mutated EGFR cancers.
  In November 2015, after a Priority Review, the US FDA granted accelerated approval to osimertinib for the treatment of metastatic epidermal growth factor receptor EGFR-T790M mutation-positive non-small cell lung cancer (NSCLC ), as detected (...)

• apatinib
  1 November 2016

  YN968D1 WKP
  Apatinib is a VEGFR2 tyrosine kinase inhibitor (VEGFR2 TKI) that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR).
  Apatinib is an orally bioavailable, small molecule agent which is thought to inhibit angiogenesis in cancer cells.
  Specifically apatinib inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. This agent also mildly inhibits c-Kit and (...)

• dacomitinib
  31 October 2016

  Targeted therapy
  non-small-cell lung cancer (NSCLC)
  EGFR tyrosine-kinase inhibitors (EGFR-TKIs or TKIs ) have now been firmly established as the first-line treatment for non-small-cell lung cancer (NSCLC) patients harboring activating EGFR mutations, based on several prospective randomized Phase III trials.
  However, despite significantly improved overall response rate and improved median progression-free survival when compared to platinum-doublet chemotherapy, EGFR-mutant NSCLC (...)

• cabozantinib
  15 October 2016

  Notes
  Cabozantinib improves ORR (46% vs 18%) & PFS (8.2 vs 5.6 months) compared with sunitinib in untreated intermediate/high-risk mRCC

• rociletinib
  15 October 2016

  rociletinib (CO-1686)
  Targeted therapy
  NSCLC Resistance to the first (erlotinib , gefitinib )- and second (afatinib )-generation EGFR-TKIs provided the rationale behind the development of the third-generation inhibitors (rociletinib , osimertinib ).
  Efficacy of rociletinib (CO-1686) in plasma-genotyped T790M-positive non-small cell lung cancer (NSCLC) patients.
  Open references
  New developments in the management of non-small-cell lung cancer, focus on rociletinib: what went wrong? (...)

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