Tipifarnib
Encyclopedia
Tipifarnib is a farnesyltransferase inhibitor
that is being investigated in patients 65 years of age and older with newly diagnosed acute myeloid leukemia
(AML). It inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive. It inhibits prenylation of the CxxX tail motif, which allows Ras to bind to the membrane where it is active. Without this step the protein cannot function.
It is also being tested in clinical trials in patients in certain stages of breast cancer.
For treatment of progressive plexiform neurofibromas associated with Neurofibromatosis type I
, it successfully passed phase one clinical trials but was suspended (NCT00029354) in phase two.
The compound was discovered by and is under investigation by Johnson & Johnson Pharmaceutical Research & Development, L.L.C, with registration number R115777.
for the treatment of AML in patients aged 65 and over with a New Drug Application (NDA) to the Food and Drug Administration (FDA) on January 24, 2005.
In June 2005, the FDA issued a "not approvable" letter for tipifarnib.
Farnesyltransferase inhibitor
The farnesyltransferase inhibitors are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras , which is commonly abnormally active in cancer....
that is being investigated in patients 65 years of age and older with newly diagnosed acute myeloid leukemia
Acute myeloid leukemia
Acute myeloid leukemia , also known as acute myelogenous leukemia, is a cancer of the myeloid line of blood cells, characterized by the rapid growth of abnormal white blood cells that accumulate in the bone marrow and interfere with the production of normal blood cells. AML is the most common acute...
(AML). It inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive. It inhibits prenylation of the CxxX tail motif, which allows Ras to bind to the membrane where it is active. Without this step the protein cannot function.
It is also being tested in clinical trials in patients in certain stages of breast cancer.
For treatment of progressive plexiform neurofibromas associated with Neurofibromatosis type I
Neurofibromatosis type I
Neurofibromatosis type I , formerly known as von Recklinghausen disease after the researcher who first documented the disorder, is a human genetic disorder. It is possibly the most common inherited disorder caused by a single gene...
, it successfully passed phase one clinical trials but was suspended (NCT00029354) in phase two.
The compound was discovered by and is under investigation by Johnson & Johnson Pharmaceutical Research & Development, L.L.C, with registration number R115777.
Approval process
Tipifarnib was submitted to the FDA by Johnson & JohnsonJohnson & Johnson
Johnson & Johnson is an American multinational pharmaceutical, medical devices and consumer packaged goods manufacturer founded in 1886. Its common stock is a component of the Dow Jones Industrial Average and the company is listed among the Fortune 500....
for the treatment of AML in patients aged 65 and over with a New Drug Application (NDA) to the Food and Drug Administration (FDA) on January 24, 2005.
In June 2005, the FDA issued a "not approvable" letter for tipifarnib.