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Crizotinib

go.drugbank.com/drugs/DB08865
ApprovedInvestigational

Crizotinib is a tyrosine kinase receptor inhibitor used for the treatment of anaplastic lymphoma kinase (ALK) or ROS1-positive non-small cell lung cancer (NSCLC) tumors, as well as ALK-positive anaplastic large cell lymphoma (ALCL) and inflammatory myofibroblastic tumor (IMT). By targeting the echinoderm microtubule...

  1. Drug

    Ceritinib

    go.drugbank.com/drugs/DB09063
    ApprovedInvestigational

    This occurrence led to development of novel second-generation ALK inhibitors such as ceritinib to overcome crizotinib resistance. … Following treatment with crizotinib (a first-generation ALK inhibitor), most tumours develop drug resistance due to mutations in key "gatekeeper" residues of the enzyme.

  2. Drug

    Lorlatinib

    go.drugbank.com/drugs/DB12130
    ApprovedInvestigational

    Lorlatinib is a third-generation ALK tyrosine kinase inhibitor (TKI) for patients with ALK-positive metastatic non-small cell lung cancer which was first approved by the US FDA in November of 2018. It was subsequently approved by the EMA...

  3. Drug

    Brigatinib

    go.drugbank.com/drugs/DB12267
    ApprovedInvestigational

    [A31311] It also exhibits selectivity against 9 different Crizotinib-resistant mutants of the EML4-ALK fusion gene, which is a pivotal player in the transformation of susceptible lung parenchyma.

  4. Drug

    Ensartinib

    go.drugbank.com/drugs/DB14860
    ApprovedInvestigational

    when compared to [crizotinib]. … [A265030] The drug is 10-fold more potent in the inhibition of the growth of ALK-positive lung cancer cell lines when compared to [crizotinib].

  5. Drug

    Repotrectinib

    go.drugbank.com/drugs/DB16826
    ApprovedInvestigational

    [A262056] ROS1 mutations are one of the defined oncogenic drives of NSCLC, and the solvent-front mutation ROS1 G2032R is responsible for 50 to 60% of [crizotinib]-resistant cases. … [A262061] Although resistance to multiple TKI has been reported, including [crizotinib], [lorlatinib], [taletrectinib], and [entrectinib], there has been no reported case of repotrectinib resistance.

  6. Drug

    Alectinib

    go.drugbank.com/drugs/DB11363
    ApprovedInvestigational

    Approved under accelerated approval in 2015, alectinib is indicated for use in patients who have progressed on or were not tolerant of crizotinib, which is associated with the development of resistance

  7. Drug

    Taletrectinib

    go.drugbank.com/drugs/DB18711
    ApprovedInvestigational

    for example, the IC50 for taletrectinib against ROS1 exhibiting the secondary solvent-front mutation _G2032R_ is 400-times lower than that of the previously approved first-generation inhibitors [crizotinib

  8. Drug

    Amivantamab

    go.drugbank.com/drugs/DB16695
    ApprovedInvestigational

    [A235103,A235118] Amivantamab was found to be more effective than the EGFR inhibitor [erlotinib] or the MET inhibitor [crizotinib] _in vivo_.