Active Ingredient History
Nilotinib (AMN107, trade name Tasigna) is a kinase inhibitor indicated for the treatment of chronic phase and accelerated phase Philadelphia chromosome-positive chronic myelogenous leukemia (CML) in adult patients resistant to or intolerant to prior therapy that included imatinib. Nilotinib is an inhibitor of the Bcr-Abl kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of Abl protein. In vitro, nilotinib inhibited Bcr-Abl mediated proliferation of murine leukemic cell lines and human cell lines derived from Ph+ CML patients. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from Bcr-Abl kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine Bcr-Abl xenograft model. Nilotinib inhibited the autophosphorylation of the following kinases at IC50 values as indicated: Bcr-Abl (20-60 nM), PDGFR (69 nM) and c-Kit (210 nM). Nilotinib is currently being trialed in people with Parkinson's disease, as it appears to be able to halt progression of the disease and even improve their symptoms. The drug also has a number of adverse effects typical of anti-cancer drugs: a headache, fatigue, gastrointestinal problems such as nausea, vomiting, diarrhea and constipation, muscle and joint pain, rash and other skin conditions, flu-like symptoms, and reduced blood cell count. Less typical side effects are those of the cardiovascular system, such as hypertension (high blood pressure), various types of arrhythmia, and prolonged QT interval. Interaction of nilotinib with OATP1B1 and OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions. Nilotinib is an inhibitor of OATP-1B1 transporter but not for OATP-1B3. Main metabolic pathways identified in healthy subjects are oxidation and hydroxylation. Nilotinib is the main circulating component in the serum. None of the metabolites contributes significantly to the pharmacological activity of nilotinib. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Alzheimer Disease (Phase 3)
Appendiceal Neoplasms (Phase 2)
Ataxia (Phase 2)
Bone Marrow Transplantation (Phase 1)
Breast Neoplasms (Phase 2)
Carcinoma, Giant Cell (Phase 2)
Cerebellar Ataxia (Phase 2)
Chondrosarcoma (Phase 1/Phase 2)
Chordoma (Phase 1)
Chronic Disease (Phase 2)
Colonic Neoplasms (Early Phase 1)
Colorectal Neoplasms (Phase 2)
Drugs, Investigational (Phase 4)
Endometrial Neoplasms (Phase 2)
Fallopian Tube Neoplasms (Phase 2)
Gastrointestinal Neoplasms (Phase 2)
Gastrointestinal Stromal Tumors (Phase 4)
Genital Neoplasms, Female (Phase 2)
Giant Cell Tumor of Tendon Sheath (Phase 2)
Glioma (Phase 2)
Graft vs Host Disease (Phase 2)
Hamartoma (Phase 2)
Head and Neck Neoplasms (Phase 1)
Healthy Volunteers (Phase 1)
Hematologic Diseases (Phase 2)
Hematopoietic Stem Cells (Phase 2)
Huntington Disease (Phase 1)
Hypereosinophilic Syndrome (Phase 1/Phase 2)
Intestinal Neoplasms (Phase 3)
Leukemia (Phase 4)
Leukemia, Lymphocytic, Chronic, B-Cell (Phase 1/Phase 2)
Leukemia, Myeloid (Phase 3)
Leukemia, Myeloid, Accelerated Phase (Phase 1/Phase 2)
Leukemia, Myeloid, Acute (Phase 2)
Leukemia, Myeloid, Chronic-Phase (Phase 4)
Leukemia, Myelomonocytic, Chronic (Phase 3)
Lewy Body Disease (Phase 2)
Lymphoma, Non-Hodgkin (Phase 1)
Lymphoma, T-Cell, Peripheral (Phase 1)
Mastocytosis, Systemic (Phase 1/Phase 2)
Melanoma (Phase 2)
Mutation (Phase 1)
Neoplasm Metastasis (Phase 2)
Neoplasm, Residual (Phase 2)
Neoplasms ()
Neurofibroma (Early Phase 1)
Neurofibromatoses (Early Phase 1)
Ovarian Neoplasms (Phase 2)
Parkinson Disease (Phase 2)
Peritoneal Neoplasms (Phase 2)
Protein-Tyrosine Kinases (Phase 1/Phase 2)
Pulmonary Arterial Hypertension (Phase 2)
Sarcoma (Phase 3)
Scleroderma, Systemic (Phase 2)
Stem Cell Transplantation (Phase 2)
Substance Withdrawal Syndrome (Phase 2)
Synovitis, Pigmented Villonodular (Phase 2)
Therapeutics (Phase 2)
Vestibular Diseases (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
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