Kinase Inhibitors

DrugDrug NameDrug Indication
DB09073PalbociclibPalbociclib is indicated in combination with [letrozole] as initial endocrine-based therapy for the treatment of human epidermal growth factor receptor type 2 (HER2)-negative and hormone receptor(HR)-positive tumors in adult patients with advanced/metastatic breast cancer. It is as well approved in combination with [fulvestrant] in patients with disease progression with prior endocrine therapy.[A176783] In the official labeling, the use of palbociclib should be accompanied with either an aromatase inhibition, no restricted to letrozole, as initial endocrine-based therapy in postmenopausal women or in man.[FDA label] The breast cancer starts as a group of cancer cells that grow into and destroy the nearby breast tissue. This growth can spread into other parts of the body which is called metastasis. According to the location of the cancer cells, it can be categorized in ductal carcinoma and lobular carcinoma. However, other types of breast cancer include inflammatory breast cancer, Paget disease of the breast, triple negative breast cancer non-Hodgkin lymphoma and soft tissue sarcoma.[L5870] In males, breast cancer is usually treated as the cases of postmenopausal women and almost all the cases are ductal carcinoma.[L5873]
DB09330OsimertinibOsimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy.
DB05239CobimetinibFor the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation. Cobimetinib is used in combination with vemurafenib, a BRAF inhibitor.
DB09054IdelalisibIdelalisib is indicated in the treatment of chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). For the treatment of relapsed CLL, it is currently indicated as a second-line agent in combination with rituximab in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities, while in the treatment of FL and SLL it is intended to be used in patients who have received at least two prior systemic therapies.
DB11363AlectinibAlectinib is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. This indication is approved under accelerated approval based on tumor response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.
DB11730RibociclibKisqali (ribociclib) is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). These proteins, when over-activated, can enable cancer cells to grow and divide too quickly. Targeting CDK4/6 with enhanced precision may play a role in ensuring that cancer cells do not continue to replicate uncontrollably.
DB11828NeratinibFor use as an extended adjuvant treatment in adult patients with early stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy [FDA Label].
DB12483CopanlisibIndicated for the treatment of adult patients with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies.
DB12001Abemaciclib* Indicated in combination with fulvestrant for the treatment of women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer with disease progression following endocrine therapy. * Inidicated as monotherapy for the treatment of adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting.
DrugDrug NameTargetType
DB09073PalbociclibCyclin-dependent kinase 4target
DB09073PalbociclibCyclin-dependent kinase 6target
DB09073PalbociclibCytochrome P450 3A4enzyme
DB09073PalbociclibSulfotransferase 2A1enzyme
DB09073PalbociclibMultidrug resistance protein 1transporter
DB09073PalbociclibATP-binding cassette sub-family G member 2transporter
DB09073PalbociclibSerum albumincarrier
DB09073PalbociclibSolute carrier family 22 member 1transporter
DB09330OsimertinibEpidermal growth factor receptortarget
DB09330OsimertinibMultidrug resistance protein 1transporter
DB09330OsimertinibATP-binding cassette sub-family G member 2transporter
DB09330OsimertinibCytochrome P450 3A4enzyme
DB09330OsimertinibCytochrome P450 1A2enzyme
DB05239CobimetinibDual specificity mitogen-activated protein kinase kinase 1target
DB05239CobimetinibCytochrome P450 3A4enzyme
DB05239CobimetinibMultidrug resistance protein 1enzyme
DB05239CobimetinibSolute carrier organic anion transporter family member 1B1transporter
DB05239CobimetinibSolute carrier organic anion transporter family member 1B3transporter
DB05239CobimetinibATP-binding cassette sub-family G member 2transporter
DB09054IdelalisibPhosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta isoform (P110δ)target
DB09054IdelalisibATP-binding cassette sub-family G member 2transporter
DB09054IdelalisibMultidrug resistance protein 1transporter
DB09054IdelalisibAldehyde oxidaseenzyme
DB09054IdelalisibUDP-glucuronosyltransferase 1A4enzyme
DB09054IdelalisibUDP-glucuronosyltransferase 1A1enzyme
DB09054IdelalisibCytochrome P450 2C8enzyme
DB09054IdelalisibCytochrome P450 2C19enzyme
DB09054IdelalisibCytochrome P450 2B6enzyme
DB09054IdelalisibCytochrome P450 3A4enzyme
DB09054IdelalisibSolute carrier organic anion transporter family member 1B1transporter
DB09054IdelalisibSolute carrier organic anion transporter family member 1B3transporter
DB09054IdelalisibCytochrome P450 3A5enzyme
DB09054IdelalisibCytochrome P450 3A43enzyme
DB09054IdelalisibCytochrome P450 3A7enzyme
DB11363AlectinibALK tyrosine kinase receptortarget
DB11363AlectinibATP-binding cassette sub-family G member 2transporter
DB11363AlectinibMultidrug resistance protein 1carrier
DB11730RibociclibCyclin-dependent kinase 4target
DB11730RibociclibCyclin-dependent kinase 6target
DB11730RibociclibCytochrome P450 3A4enzyme
DB11828NeratinibCytochrome P450 3A4enzyme
DB11828NeratinibDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB11828NeratinibMultidrug resistance protein 1transporter
DB11828NeratinibEpidermal growth factor receptortarget
DB11828NeratinibSerum albumincarrier
DB11828Neratinibalpha1-acid glycoproteincarrier
DB12483CopanlisibPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformtarget
DB12483CopanlisibPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformtarget
DB12483CopanlisibCytochrome P450 3A4enzyme
DB12483CopanlisibCytochrome P450 3A5enzyme
DB12483CopanlisibCytochrome P450 3A7enzyme
DB12483CopanlisibCytochrome P450 3A43enzyme
DB12483CopanlisibMultidrug resistance protein 1transporter
DB12483CopanlisibATP-binding cassette sub-family G member 2transporter
DB12483CopanlisibMultidrug and toxin extrusion protein 2transporter
DB12483CopanlisibSerum albumincarrier
DB12001AbemaciclibMultidrug and toxin extrusion protein 1transporter
DB12001AbemaciclibMultidrug and toxin extrusion protein 2transporter
DB12001AbemaciclibCyclin-dependent kinase 4target
DB12001AbemaciclibCyclin-dependent kinase 6target
DB12001AbemaciclibSerum albumincarrier
DB12001Abemaciclibalpha1-acid glycoproteincarrier
DB12001AbemaciclibCytochrome P450 3A4enzyme
DB12001AbemaciclibOrnithine carbamoyltransferase, mitochondrialtransporter
DB12001AbemaciclibMultidrug resistance protein 1transporter
DB12001AbemaciclibATP-binding cassette sub-family G member 2transporter