ARIAD announces initial results from AP26113 Phase 1/2 trial on non-small cell lung cancer

We know that, AP26113 (see structure) is a highly potent ALK inhibitor with IC50 of 0.62 nM. As an ALK inhibitor, AP26113 overcomes mutation-based resistance in NSCLC models. Multiple mutations in ALK were identified that conferred resistance to crizotinib, but not AP26113, including the L1196M "gatekeeper" mutation which has now been observed clinically in patients who initially responded to crizotinib and then relapsed. AP26113 also inhibits activated EGFR in preclinical models, including the T790M "gatekeeper" mutant that confers resistance to current EGFR inhibitors. Constitutive EGFR activity due to activating mutation is a key feature of certain non-small cell lung cancers, and the T790M mutation causes resistance to inhibitor therapy in approximately 50 percent of these cases. In preclinical studies, AP26113 was shown to be specific for mutated EGFR and avoids inhibition of native (endogenous or unmutated) EGFR; such inhibition is thought to be associated with the toxicity of other EGFR inhibitors.

ARIAD announces initial results from AP26113 Phase 1/2 trial on non-small cell lung cancer

Scientists develop new strategy to overcome drug-resistant childhood cancer

Researchers at The Institute of Cancer Research in London have found a way to overcome the resistance of cancer cells to a drug called crizotinib, which recently showed positive early results in its first trial in children with cancer.

Crizotinib (see structure) has already been licensed by the US Food and Drug Administration for use in adult cancers, but early experience suggests tumours eventually stop responding to treatment, after developing additional mutations in the ALK gene targeted by the drug.

Xalkori Helps Lung Cancer Patients | News | Drug Discovery and Development Magazine

In continuation of my update Crizotinib/Xalkori 

Pfizer Inc. said its lung cancer drug Xalkori helped lung cancer patients who had previously been treated for the disease.

Pfizer said Xalkori (see the structre)  worked better than two older cancer drugs in the late-stage clinical trial. All patients had a rare type of non-small cell lung cancer and had previously been treated. The Food and Drug Administration approved Xalkori in August for use in patients whose cancer had not been treated.

In the study, patients took Xalkori, Alimta, or Taxotere. Pfizer said patients who took Xalkori had greater progression-free survival, or time from the start of treatment until they died or experienced disease progression. Xalkori is a pill taken twice per day while Alimta and Taxotere are given intravenously.

Xalkori is approved for use against non-small cell lung cancer in patients who have an abnormal gene that causes tumor growth. Xalkori blocks that gene, which is found in 1 percent to 7 percent of non-small cell lung cancer. About 85 percent of lung cancers are the non-small cell variety...

More...

Xalkori Helps Lung Cancer Patients | News | Drug Discovery and Development Magazine

Experimental Drug Helps Fight Some Childhood Cancers, Study Finds

In continuation of my update on Crizotinib

Experimental Drug Helps Fight Some Childhood Cancers, Study Finds:  A new targeted drug therapy may help treat certain advanced cancers in children, a new preliminary study indicates.In some cases, the oral medication even made tumors disappear after regular cancer treatments had failed, the...

Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

In continuation of my update on Crizotinib.....
Press Announcements FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer

EMA has accepted Pfizer's regulatory submissions for review of two investigational compounds crizotinib and bosutinib

European Medicines Agency (EMA) has accepted Pfizer's regulatory submissions for review of two investigational compounds  crizotinib, an oral first-in-class anaplastic lymphoma kinase (ALK) inhibitor, for the treatment of patients with previously treated ALK-positive advanced non-small cell lung cancer (NSCLC); and bosutinib for the treatment of adult patients with newly diagnosed Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) in the chronic phase. 

Crizotinib

                                                                                               Bosutinib

Dr. Andreas Penk, president of Pfizer Oncology Europe, claims that,

"With the EMA submissions for crizotinib and bosutinib, we are one step closer to potentially bringing two promising agents to patient populations in areas of significant unmet medical need"......

Crizotinib Shows Dramatic Results for Shrinking Tumors (lung cancer)....

Patients with a specific kind of lung cancer may benefit from a Phase III clinical trial offered by the Moores UCSD Cancer Center. The new drug, crizotinib (structure), under development by Pfizer, showed dramatic results in reducing lung cancer tumors in some patients during Phase I and II clinical trials.

"The results of the first two trials have been very encouraging," said Lyudmila Bazhenova, MD, assistant clinical professor at UC San Diego School of Medicine and a member of the Moores UCSD Cancer Center...

According to a preliminary study,  57% of patients had their tumors reduced and at eight weeks of the treatment, 87% showed disease stabilization.

The Phase III clinical trial will compare crizotinib with standard-of-care chemotherapy in the treatment of ALK-positive recurrent NSCLC. Through a randomized selection process, patients will either be treated with chemotherapy or crizotinib. If the patients who are given the chemotherapy do not respond to treatment, they will be given crizotinib at the end of the trial....

Ref : http://ucsdnews.ucsd.edu/newsrel/health/06-22ShrinkingTumors.asp