Protein Kinase Inhibitors
- Name
- Protein Kinase Inhibitors
- Accession Number
- DBCAT000737
- Description
Agents that inhibit PROTEIN KINASES.
- ATC Classification
- Drugs
Drug Drug Description Gefitinib A tyrosine kinase inhibitor used as first-line therapy to treat non-small cell lung carcinoma (NSCLC) that meets certain genetic mutation criteria. Sorafenib A kinase inhibitor used to treat unresectable liver carcinoma, advanced renal carcinoma, and differentiated thyroid carcinoma. Erlotinib An EGFR tyrosine kinase inhibitor used to treat certain small cell lung cancers or advanced metastatic pancreatic cancers. Imatinib A tyrosine kinase inhibitor used to treat a number of leukemias, myelodysplastic/myeloproliferative disease, systemic mastocytosis, hypereosinophilic syndrome, dermatofibrosarcoma protuberans, and gastrointestinal stromal tumors. Dasatinib A tyrosine kinase inhibitor used for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia or chronic myeloid leukemia. Lapatinib An antineoplastic agent and tyrosine kinase inhibitor used for the treatment of advanced or metastatic HER-positive breast cancer in patients who received prior chemotherapeutic treatments. Temsirolimus A antineoplastic agent used in the treatment of renal cell carcinoma (RCC) that works by inhibiting mTOR. Axitinib An oral VEGFR and kinase inhibitor used for the treatment of advanced renal cell carcinoma after failure of one prior systemic therapy. Crizotinib A receptor tyrosine kinase inhibitor used to treat metastatic non-small cell lung cancer (NSCLC) where the tumors have been confirmed to be anaplastic lymphoma kinase (ALK), or ROS1-positive. Ponatinib A kinase inhibitor used to treat patients with various types of chronic myeloid leukemia (CML). Trametinib A kinase inhibitor used alone or in combination with dabrafenib to treat patients with cancers with specific BRAF mutations, such as melanoma and non-small cell lung cancer. Dabrafenib A kinase inhibitor used to treat patients with specific types of melanoma, non-small cell lung cancer, and thyroid cancer. Ceritinib An antineoplastic kinase inhibitor used to treat anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) in patients with inadequate clinical response or intolerance to crizotinib. Palbociclib An endocrine-based chemotherapeutic agent used in combination with other antineoplastic agents to treat HER2-negative and HR-positive advanced or metastatic breast cancer. Lenvatinib A receptor tyrosine kinase inhibitor used for the treatment of metastatic thyroid cancer, advanced renal cell carcinoma in combination with everolimus, and unresectable hepatocellular carcinoma. Masitinib Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in dogs. It has been available in Europe since 2009, under the brand name Masivet. In the... Cediranib For the treatment of liver cancer, advanced non-small cell lung cancer (NSCLC), advanced colorectal cancer (CRC) and other solid tumors. Genistein Currently Genistein is being studied in clinical trials as a treatment for prostate cancer. 7-Hydroxystaurosporine Not Available Alvocidib Investigated for use/treatment in esophageal cancer, leukemia (lymphoid), lung cancer, liver cancer, and lymphoma (unspecified). Vatalanib Used in combination with first- and second-line chemotherapy for the treatment of metastatic colorectal cancer and non-small cell lung cancer (NSCLC). AT9283 Investigated for use/treatment in cancer/tumors (unspecified), leukemia (myeloid), and solid tumors. CYC116 Advanced solid tumors Alisertib For the treatment of various forms of cancer. MKC-1 Investigated for use/treatment in breast cancer, leukemia (unspecified), lung cancer, and solid tumors. SNS-314 Investigated for use/treatment in solid tumors. Seliciclib Investigated for use/treatment in breast cancer, lung cancer, lymphoma (unspecified), multiple myeloma, leukemia (lymphoid), and cancer/tumors (unspecified). Semaxanib Investigated for use/treatment in colorectal cancer and lung cancer. Midostaurin An antineoplastic agent used to treat high-risk acute myeloid leukemia (AML) with specific mutations, aggressive systemic mastocytosis (ASM), systemic mastocytosis with associated hematologic neoplasm (SM-AHN), or mast cell leukemia (MCL). Tofacitinib A Janus kinase (JAK) inhibitor used to treat rheumatic conditions, such as rheumatoid arthritis and ankylosing spondylitis, and ulcerative colitis. Osimertinib A tyrosine kinase inhibitor used in the treatment of certain types of non-small cell lung carcinoma. Alectinib A kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Rabusertib Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non Small Cell Lung Cancer. Barasertib Barasertib has been used in trials studying the treatment of Tumors, Lymphoma, Solid Tumors, Solid Tumours, and Myeloid Leukemia, among others. Spebrutinib Spebrutinib has been used in trials studying the treatment of Rheumatoid Arthritis, Lymphoma, Large B-Cell, Diffuse, and Leukemia Lymphocytic Chronic B-Cell. Danusertib Danusertib has been used in trials studying the treatment of Leukemia. Bafetinib Bafetinib has been used in trials studying the treatment of Adult Gliosarcoma, Adult Mixed Glioma, Adult Glioblastoma, Chronic Myeloid Leukemia, and Acute Lymphocytic Leukemia, among others. Flumatinib Flumatinib has been used in trials studying the treatment of Myelogenous Leukemia, Chronic. Vistusertib Vistusertib is under investigation for the treatment of Advanced Gastric Adenocarcinoma. Orantinib Orantinib has been used in trials studying the treatment of Lung Cancer, Breast Cancer, Kidney Cancer, Gastric Cancer, and Prostate Cancer, among others. Losmapimod Losmapimod has been investigated for the prevention of Chronic Obstructive Pulmonary Disease. Indirubin Indirubin is under investigation in clinical trial NCT01735864 (Dosage Determination Trial for Indigo Naturalis Extract in Oil Ointment). Merestinib Merestinib has been used in trials studying the treatment of Cancer, Solid Tumor, Advanced cancer, ColoRectal Cancer, and Metastatic Cancer, among others. MK-5108 MK-5108 has been used in trials studying the treatment of Cancer, Neoplasms, Tumors. TAK-901 TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others. PF-03814735 PF-03814735 has been used in trials studying the treatment of Solid Tumors. Sunitinib A receptor tyrosine kinase inhibitor and chemotherapeutic agent used for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Nilotinib A kinase inhibitor used for the chronic phase treatment of Chronic Myeloid Leukemia (CML) that is Philadelphia chromosome positive and for the treatment of CML that is resistant to therapy containing imatinib. Vandetanib An antineoplastic kinase inhibitor used to treat symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. Ridaforolimus Investigated for use/treatment in solid tumors, sarcoma, cancer/tumors (unspecified), endometrial cancer, prostate cancer, and bone metastases. Pazopanib An antineoplastic agent used in the treatment of advanced renal cell cancer and advanced soft tissue sarcoma in patients with prior chemotherapy. Bosutinib An antineoplastic agent used for the treatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) in adults with inadequate clinical response to other treatments. Cabozantinib A tyrosine kinase inhibitor used to treat advanced renal cell carcinoma, hepatocellular carcinoma, and medullary thyroid cancer. Ruxolitinib A kinase inhibitor used to treat various types of myelofibrosis, polycythemia vera in patients who have not responded to or cannot tolerate hydroxyurea, and to treat graft-versus-host disease in cases that are refractory to steroid treatment. Vemurafenib A kinase inhibitor used to treat patients with Erdheim-Chester Disease who have the BRAF V600 mutation, and melanoma in patients who have the BRAF V600E mutation. Regorafenib A kinase inhibitor used to treat patients with metastatic colorectal cancer, unresectable, locally advanced, or metastatic gastrointestinal stromal tumors, and hepatocellular carcinoma. Afatinib An antineoplastic agent used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with non-resistant EGFR mutations or resistance to platinum-based chemotherapy. Ibrutinib An antineoplastic agent used to treat chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's Macroglobulinemia. Nintedanib A triple angiokinase inhibitor indicated for the treatment of idiopathic pulmonary fibrosis, systemic sclerosis-associated interstitial lung disease, and in combination with docetaxel for non-small cell lung cancer. Tivozanib A kinase inhibitor to treat adult patients with renal cell carcinoma (RCC) who have failed prior systemic therapies or experienced relapsed disease. Wortmannin Wortmannin is a steroid metabolite of Penicillium funiculosum and Talaromyces wortmannii fungi. This drug acts as a nonspecific, covalent inhibitor of phosphoinositide 3-kinase enzymes (PI3Ks). Everolimus A mammalian target of rapamycin (mTOR) kinase inhibitor used to treat various types of malignancies. Mangostin Mangostin is a plant/plant extract used in some OTC (over-the-counter) products. It is not an approved drug. Sirolimus An mTOR inhibitor immunosuppressant used to prevent organ transplant rejections, treat lymphangioleiomyomatosis, and treat adults with perivascular epithelioid cell tumors. Emodin Emodin has been investigated for the treatment of Polycystic Kidney. Fasudil Fasudil has been investigated in Carotid Stenosis. MLN8054 MLN8054 has been used in trials studying the treatment of Colon Neoplasm, Breast Neoplasm, Bladder Neoplasm, Pancreatic Neoplasm, and Advanced Malignancies. Cobimetinib An antineoplastic agent and selective inhibitor of the mitogen-activated extracellular kinase (MEK) pathway used to treat unresectable or metastatic melanoma. Encorafenib A kinase inhibitor used to treat unresectable or metastatic melanoma with specific mutations. Ribociclib A kinase inhibitor used to treat HR+, HER2- advanced or metastatic breast cancer. Icotinib Icotinib hydrochloride is a novel epidermal growth factor receptor (EGFR)–tyrosine kinase inhibitor, exhibits encouraging efficacy and tolerability in patients with advanced non-small-cell lung cancer (NSCLC) who failed previous chemotherapy. Neratinib A protein kinase inhibitor used to treat breast cancer that over expresses the HER2 receptor. Rociletinib Rociletinib has been used in trials studying the treatment and prevention of Nonsmall Cell Lung Cancer, Non-small Cell Lung Cancer, and Locally Advanced or Metastatic Non-small Cell Lung Cancer. Dacomitinib A medication used to treat non small cell lung cancer with EGFR exon 19 deletion of exon 21 L858R substitution. Binimetinib A medication used to treat metastatic melanoma with specific mutations. Abemaciclib A medication used to treat HR+ HER2- advanced or metastatic breast cancer. Lorlatinib An anaplastic lymphoma kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Brigatinib An anaplastic lymphoma kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Olmutinib For use in treatment of metastatic T790M mutation positive non-small cell lung cancer . Pimasertib Pimasertib is under investigation in clinical trial NCT01378377 (Combination Trial of Pimasertib (MSC1936369B) With Temsirolimus). Avutometinib Avutometinib (RO-5126766 free base) is under investigation in clinical trial NCT03875820 (Phase I Trial of VS-6063 and RO5126766.). Pelitinib Investigated for use/treatment in colorectal cancer and lung cancer. Motesanib Investigated for use/treatment in solid tumors. AV-412 Investigated for use/treatment in cancer/tumors (unspecified). Ilorasertib Ilorasertib has been used in trials studying the treatment of Myelodysplasia, Solid Neoplasm, Advanced Cancers, Advanced Solid Tumors, and Acute Myelogenous Leukemia, among others. Momelotinib A Janus Kinase inhibitor used to treat intermediate or high-risk myelofibrosis. GSK-2636771 GSK2636771 has been used in trials studying the treatment of CANCER, LYMPHOMA, Solid Neoplasm, Recurrent Solid Neoplasm, and Advanced Malignant Neoplasm, among others. Gedatolisib Gedatolisib has been used in trials studying the basic science and treatment of Neoplasm, Ovary Cancer, Breast Cancer, Advanced Cancer, and Endometrial Cancer, among others. Tesevatinib Tesevatinib has been used in trials studying the treatment of Cancer, Stomach Cancer, Brain Metastases, Esophageal Cancer, and Leptomeningeal Metastases, among others. Tesevatinib is a potent inhibitor of multiple RTKs... Entrectinib Entrectinib is indicated for the treatment of metastatic ROS1-positive non-small cell lung cancer in adults. Entrectinib is also indicated in adults and children over 12 years old for the treatment... Naquotinib Naquotinib has been used in trials studying the treatment of Solid Tumors, Non-small Cell Lung Cancer, Non-Small-Cell Lung Cancer (NSCLC), Epidermal Growth Factor Receptor Mutations, and Epidermal Growth Factor Receptor... Rigosertib Rigosertib has been used in trials studying the treatment and basic science of MDS, RAEB, Cancer, Hepatoma, and Neoplasms, among others. Rimacalib Rimacalib has been used in trials studying the treatment of Rheumatoid Arthritis (RA). Rebastinib Rebastinib has been used in trials studying the treatment of Chronic Myeloid Leukemia. It is an inhibitor of Tie2 tyrosine kinase receptor and an antineoplastic agent. AZD-0424 AZD0424 has been used in trials studying the treatment of Advanced Solid Tumours. X-396 X-396 has been used in trials studying the treatment of Advanced Solid Tumors and Non-small Cell Lung Cancer. Rivoceranib Rivoceranib is under investigation in clinical trial NCT02726854 (Apatinib as Second-line Treatment of Advanced Pancreatic Cancer). Ensartinib Ensartinib is under investigation in clinical trial NCT03420508 (Treating Patients With Melanoma and ALK Alterations With Ensartinib). PF-06700841 PF-06700841 is under investigation in clinical trial NCT03236493 (Safety and Pharmacokinetic Study of PF-06700841 in Japanese Healthy Volunteers). Zanubrutinib A kinase inhibitor used to treat mantle cell lymphoma, a type of B-cell non-Hodgkin lymphoma, in adults who previously received therapy. Upadacitinib An oral Janus kinase (JAK)1-selective inhibitor used in the treatment of moderate to severe rheumatoid arthritis, active psoriatic arthritis, ankylosing spondylitis, and severe atopic dermatitis, including in patients who did not respond well to other therapies. Voruciclib Voruciclib is under investigation in clinical trial NCT03547115 (A Phase 1 Study of Voruciclib in Subjects With B-Cell Malignancies or AML). Abivertinib Abivertinib is a tyrosine kinase inhibitor targeted against mutant forms of both human epidermal growth factor receptor (EGFR) and Bruton's tyrosine kinase (BTK). It has been investigated for use in... Avapritinib A selective tyrosine kinase inhibitor being investigated for the treatment of multidrug resistant gastrointestinal tumors. H-89 Not Available Doramapimod Doramapimod is a P38 MAP kinase inhibitor. AKI-001 AKI-001 is an aurora kinase inhibitor. Reversine Not Available Dorsomorphin Not Available AZD-8330 Investigated for use/treatment in cancer/tumors (unspecified). (Rp)-cAMPS Not Available Ripretinib A kinase inhibitor used to treat advanced gastrointestinal stromal tumor (GIST). Acalabrutinib A Bruton tyrosine kinase inhibitor used to treat mantle cell lymphoma, chronic lymphocytic leukemia, and small lymphocytic lymphoma. Gilteritinib An AXL receptor tyrosine kinase inhibitor used to treat relapsed or refractory acute myeloid leukemia. Fedratinib Fedratinib is indicated for the treatment of adult patients with intermediate-2 or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis.[L8090,L47016] Quizartinib A FLT3 inhibitor used in combination with cytarabine and anthracycline to treat acute myeloid leukemia with FLT3 internal tandem duplication Larotrectinib A kinase inhibitor used to treat solid tumors with neurotrophic receptor tyrosine kinase gene fusion, are metastatic, high risk for surgery, or have no alternative treatments. FF-10101-01 FF-10101-01 is under investigation in clinical trial NCT03194685 (Study of FF-10101-01 in Patients With Relapsed or Refractory Acute Myeloid Leukemia). Acrizanib Acrizanib is under investigation in clinical trial NCT02355028 (LHA510 Proof-of-concept Study as a Maintenance Therapy for Patients With Wet Age-related Macular Degeneration). Nemiralisib Nemiralisib is under investigation in clinical trial NCT03345407 (Dose Finding Study of Nemiralisib (GSK2269557) in Subjects With an Acute Moderate or Severe Exacerbation of Chronic Obstructive Pulmonary Disease (COPD)). Tepotinib An oral tyrosine kinase inhibitor targeted against MET for the treatment of metastatic non-small cell lung cancer in patients exhibiting MET exon 14 skipping mutations. Trilaciclib A CDK4 and CDK6 inhibitor to reduce the risk of chemotherapy induced myelosuppression. Umbralisib A kinase inhibitor used to treat rare forms of refractory lymphoma. Deucravacitinib A TYK2 inhibitor being investigated as a treatment for psoriasis. Tucatinib A kinase inhibitor used to treat certain types of unresectable/metastatic HER-2 positive breast cancer. Prexasertib Prexasertib has been used in trials studying the treatment and basic science of mCRPC, Leukemia, Neoplasm, breast cancer, and Ovarian Cancer, among others. PF-477736 PF-00477736 has been used in trials studying the treatment of Neoplasms. Nedisertib Nedisertib is under investigation in clinical trial NCT03770689 (Study of M3814 in Combination With Capecitabine and Radiotherapy in Rectal Cancer). Belumosudil An oral inhibitor of rho-associated coiled-coil-containing protein kinases (ROCK) used in the treatment of chronic graft-versus-host disease (GVHD). Ipatasertib Ipatasertib has been used in trials studying the treatment of Cancer, Neoplasms, Solid Cancers, Breast Cancer, and Gastric Cancer, among others. Selonsertib Selonsertib is under investigation in clinical trial NCT03053050 (Safety and Efficacy of Selonsertib in Adults With Nonalcoholic Steatohepatitis (NASH) and Bridging (F3) Fibrosis). Abrocitinib A kinase inhibitor used to treat moderate-to-severe atopic dermatitis in adults. Agerafenib Agerafenib is under investigation in clinical trial NCT03052569 (Expanded Access to RXDX-105 for Cancers With RET Alterations). Onvansertib Onvansertib is under investigation in clinical trial NCT03303339 (Onvansertib in Combination With Either Low-dose Cytarabine or Decitabine in Adult Patients With Acute Myeloid Leukemia (AML).). Vorolanib Vorolanib is under investigation in clinical trial NCT03904719 (CM082 and JS001 in Patients With Advanced Small-cell Lung Cancer (SCLC)). Ravoxertinib Ravoxertinib is under investigation in clinical trial NCT01875705 (A Dose-Escalation Study of GDC-0994 in Patients With Locally Advanced or Metastatic Solid Tumors). Vactosertib Vactosertib is under investigation in clinical trial NCT03724851 (Vactosertib in Combination With Pembrolizumab in Metastatic Colorectal or Gastric Cancer). Branebrutinib Branebrutinib is under investigation in clinical trial NCT02705989 (Safety, Tolerability and Relative Bioavailability Study of BMS-986195 in Healthy Subjects). Acumapimod Acumapimod is under investigation in clinical trial NCT02926326 (The Effect of Azithromycin on BCT197 Exposure in Healthy Male Volunteers). Alflutinib Alflutinib is under investigation in clinical trial NCT03452592 (Efficacy and Safety of Alflutinib in Locally Advanced or Metastatic Non-small Cell Lung Cancer Patients With T790M). Chiauranib Chiauranib is under investigation in clinical trial NCT03974243 (Chiauranib in Combination With Chidamide in Patients With Relapsed/refractory Non-hodgkin's Lymphoma). Lazertinib Lazertinib is under investigation in clinical trial NCT04487080 (A Study of Amivantamab and Lazertinib Combination Therapy Versus Osimertinib in Locally Advanced or Metastatic Non-small Cell Lung Cancer). AZD-7648 Not Annotated ENMD-981693 Not Annotated Idelalisib An antineoplastic kinase inhibitor used to treat chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). Selumetinib A MEK 1/2 inhibitor used in pediatric patients to treat neurofibromatosis type 1 (NF1) accompanied by symptomatic, inoperable plexiform neurofibromas (PN). Pacritinib A kinase inhibitor used for the treatment of primary and secondary myelofibrosis in adult patients with significantly reduced platelet counts. Capmatinib A kinase inhibitor targeting c-Met receptor tyrosine kinase in the treatment of non-small cell lung cancer with MET exon 14 skipping. Infigratinib An FGFR inhibitor used to treat locally advanced or metastatic cholangiocarcinoma in adults with a fibroblast growth factor receptor 2 (FGFR2) rearrangement. Duvelisib An inhibitor of phosphatidylinositol 3-kinase delta and gamma used to treat relapsed or refractory chronic lymphocytic leukemia or small lymphocytic lymphoma. Alpelisib Alpelisib is indicated in combination with fulvestrant to treat postmenopausal women, and men, with advanced or metastatic breast cancer. This cancer must be hormone receptor (HR)-positive, human epidermal growth factor... Erdafitinib A fibroblast growth factor receptor tyrosine kinase inhibitor used to treat locally advanced or metastatic urothelial carcinoma. Copanlisib A PI3K inhibitor used to treat relapsed follicular lymphoma in adults. Asciminib An inhibitor of ABL/BCR-ABL1 tyrosine kinase for the treatment of patients with Philadelphia chromosome-positive CML, including those with the T315I mutation. Pexidartinib An antitumor agent that is used for the treatment of rare disease tenosynovial giant cell tumors (TGCT) by inhibiting colony-stimulating factor 1 and its receptor. Pemigatinib A kinase inhibitor used to treat locally advanced or metastatic, unresectable cholangiocarcinoma in previously treated adult patients. Futibatinib A kinase inhibitor used to treat intrahepatic cholangiocarcinoma in previously treated adults. Selpercatinib A RET receptor tyrosine kinase inhibitor for the treatment of RET-driven non-small cell lung cancer, medullary thyroid cancer, and thyroid cancer in appropriate patient populations. Pralsetinib A RET receptor tyrosine kinase inhibitor for the treatment of metastatic RET-driven non-small cell lung cancer. PD-98059 PD-98059 is an inhibitor of MAP-kinase kinase activation. TPCA-1 TPCA-1 is a selective inhibitor of human IκB kinase 2 (IKK-2). KX-2361 Not Annotated AMG-900 Not Annotated ONO-7579 Not Annotated Pirtobrutinib A kinase inhibitor used to treat relapsed or refractory mantle cell lymphoma (MCL) after at least two lines of systemic therapy. Remibrutinib Not Annotated Parsaclisib Parsaclisib is under investigation in clinical trial NCT03126019 (An Open-Label Study of Parsaclisib in Relapsed or Refractory Follicular Lymphoma (CITADEL-203)). Surufatinib Surufatinib is under investigation in clinical trial NCT02588170 (Phase III Study of Surufatinib in Treating Advanced Extrapancreatic Neuroendocrine Tumors). Mobocertinib An oral kinase inhibitor targeted against EGFR and used in the treatment of NSCLC with EGFR exon 20 insertion mutations. 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine Not Annotated AUM-302 Not Annotated - Drugs & Drug Targets