To remind us that pharma's sometimes develop innovative drugs all by themselves <g>, here is an announcement by JNJ today on their oral Farnesyl transferase inhibitor:
UPDATE - J&J says leukemia drug eliminated signs of cancer
Tuesday July 15, 12:08 pm ET
NEW YORK, July 15 (Reuters) - Johnson & Johnson (NYSE:JNJ - News) on Tuesday said its experimental leukemia drug Zarnestra eliminated all signs of cancer in 30 percent of elderly patients treated with the medicine.
J&J said the drug also prolonged lives considerably. The average elderly patient taking Zarnestra survived 227 days, versus only 77 days in patients taking a standard chemotherapy drug, it told analysts at a meeting in New York where it reviewed its pipeline of experimental medicines.
The diversified health care company said 30 percent of elderly patients with acute myelogenous leukemia given Zarnestra in a clinical trial saw "complete responses," meaning all signs of cancer disappeared.
Acute myelogenous leukemia is the most common type of leukemia in adults, in which immune-system cells become cancerous and rapidly replace normal cells in the bone marrow. People over age 60 have the poorest chance of responding to treatment, which is meant to destroy all leukemia cells.
Officials of New Brunswick, New Jersey-based J&J said it has already discussed the results with the U.S. Food and Drug Administration (News - Websites).
"Regulatory authorities share our excitement about the results," one J&J official said, noting that additional testing will be needed to confirm the drug's safety and effectiveness.
Company officials said they were also encouraged by early trials of a medicine that could become the successor to the company's blockbuster Risperdal treatment for schizophrenia, and possibly also treat bipolar disorder, depression and anxiety.
J&J officials said the once-daily experimental anti-psychotic apparently does not cause the worrisome weight gains that have recently caused a slowdown in sales growth of Zyprexa, Eli Lilly and Co.'s (NYSE:LLY - News) top-selling rival schizophrenia drug.
J&J officials said they plan to seek U.S. approval by year's end for a new medical device called E Trans meant to treat pain following operations.
The company plans to seek U.S. approval early next year for its experimental skin patch for pain. called AP 48, which it billed as the successor to its popular Duragesic pain patch.
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Here is some more on the drug (from a multiple myeloma site):
Full Name:
Zarnestra® (tipifarnib)
Other Names:
R115777, FTI
Description:
Farnesyl transferase inhibitor (oral)
Phase:
II
Company:
Johnson and Johnson Pharmaceutical Research and Development
What It Is
Zarnestra is a novel targeted anticancer therapy under development for use in the treatment of myeloma and other cancers.
How It Works
Overview
Zarnestra is 1 of a group of drugs known as farnesyl transferase inhibitors (FTIs). FTIs inhibit an enzyme known as farnesyl transferase, which is needed for the activation of a growth-promoting gene called ras. FTIs inhibit the growth of various cancer cells.
Details About Zarnestra's Mechanism of Action
The ras gene acts somewhat like a growth "on-off" switch. Genetic mutations can occur in ras, which keep it in the "on" position and stimulate cells to keep growing. These ras mutations are found in about 30% of all human cancers and are among the most common cancer gene mutations found in multiple myeloma. Patients with a mutated ras gene are less likely to respond to chemotherapy and tend to have a poorer prognosis than patients without the mutation.
Cell growth signals are transmitted by the activation of ras within the cell. To become activated, ras must become embedded in the cell membrane. But before ras can do this, it must first be altered. An enzyme known as farnesyl transferase alters ras so that it can locate in the cell membrane. Zarnestra inhibits farnesyl transferase; thus ras cannot be altered, and it cannot locate in the cell membrane. Therefore, ras is not activated and the signal for cell growth is not transmitted.
How It Is Administered
Zarnestra is given orally, twice a day.
Potential Side Effects
In the ongoing Phase II study in myeloma, Zarnestra has been well tolerated. The most commonly reported side effect to date has been fatigue, the severity of which appears to be dose-related. Other side effects reported include diarrhea, nausea, neuropathy (a disorder of the nerves that can result in abnormal sensations, such as burning or tingling, in the hands and feet), anemia, and low platelet counts.
Preclinical Studies
In the laboratory, Zarnestra has been shown to inhibit the growth of myeloma cell lines and to induce apoptosis (programmed cell death). It also induced apoptosis in myeloma cells from patients. Zarnestra appears to interrupt various signaling pathways that are involved in myeloma cell survival and growth.
Clinical Trials
Zarnestra has been shown to have antimyeloma activity in clinical trials. It is currently being evaluated in Phase II trials.
Phase II
The clinical activity of Zarnestra was previously evaluated in a Phase II trial in patients with various hematological malignancies, including myeloma. Patients received 600 mg of Zarnestra orally twice daily for 4 weeks, followed by 2 weeks off (1 cycle). Of the patients with myeloma in the study, 1 had a reduction in M protein of 34%. (Cortes et al. Blood. 0 (2002):200207197. [epub ahead of print])
Zarnestra is currently being evaluated in a Phase II trial in patients with relapsed or refractory myeloma. Patients receive oral Zarnestra 2 times a day for 3 weeks, followed by 1 week off (1 cycle). Patients receive 2 cycles of therapy and continue on therapy if they improve or have stable disease.
In April 2002, preliminary results on 12 of the 20 patients enrolled in the trial at the time were reported at the American Association of Cancer Research Meeting in San Francisco, CA. At that time, 50% of the patients had a reduction in M protein of less than 25%, meaning they had stable disease.
Results thus far indicate that Zarnestra is well tolerated. Four of the 6 patients with stable disease had received 4 or more treatment cycles without significant toxicity. The most common side effect seen was fatigue, which was reported in 75% of patients. The severity of fatigue appeared to be dose-related. Other side effects reported were diarrhea, nausea, neuropathy, anemia, and low platelet counts.
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Note that OSI at one stage had a Farnesyl transferase inhibitor in the clinic - I believe it was returned to them by Pfizer and I don't know what (if anything) they have done with it.
Peter |
