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Pharmas and Dx Partners Race to Launch the First Personalized EGFR Inhibitor for Lung Cancer

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This article has been updated from an earlier version with additional information from Qiagen on its PMA filing for an EGFR mutation companion test.

A race commenced this week between Boehringer Ingelheim and Roche to launch the first pharmacogenetically targeted EGFR inhibitor for non-small cell lung cancer in the US market.

Boehringer and Qiagen on Jan. 15 simultaneously announced that they had submitted applications to the US Food and Drug Administration for the marketing approval of afatinib, a new EGFR inhibitor for the treatment of non-small cell lung cancer, and a companion test to pick out best responders to the drug. The companies told PGx Reporter that the NDA and the PMA had been submitted to the FDA in the fourth quarter of 2012.

A day after Boehringer and Qiagen made their announcement, Astellas announced that it had submitted a supplemental NDA for Tarceva (erlotinib) for first-line treatment of NSCLC and that Roche had at the same time submitted a companion EGFR mutation test to pick out best responders to the drug. Astellas, an affiliate of OSI Pharmaceuticals, and Roche subsidiary Genentech jointly market Tarceva in the US.

Both Tarceva and afatinib have received Priority Review designations from the FDA, placing them on a six-month review clock. In the ideal scenario, the agency will approve the drug and test on the same day to ensure that lung cancer patients have access to an FDA-approved test that can predict whether they will respond to the drug.

In the past, the agency has beat its own review deadlines for personalized medicine products such as Roche's Zelboraf and its companion BRAF genetic test, and Pfizer's Xalkori and its accompanying ALK test. For example, after the FDA accepted Xalkori's NDA and Abbott's premarket approval for the companion FISH test, it took the agency just over three months to issue a positive decision on the combination product (PGx Reporter 9/7/2011).

Once on the market, Boehringer's afatinib will likely compete with Tarceva in the US market, where it is already approved as a second- or third-line treatment for advanced NSCLC. In 2011, Tarceva brought in more than $1 billion in worldwide sales.

However, afatinib is distinguished from first-generation EGFR inhibitors such as Tarceva and Iressa in that it is an irreversible inhibitor. Boehringer is hoping that the drug will be more effective than these earlier products. Afatinib covalently binds to EGFR, HER2, and HER4 receptors that are overexpressed in certain cancers. Once the drug permanently attaches to the cell receptors, it blocks these receptors and inhibits cell signaling pathways that cause tumor cells to proliferate.

Afatinib

Boehringer is seeking approval for afatinib as a treatment for patients with locally advanced or metastatic NSCLC who harbor a mutation in the EGFR gene. Meanwhile, Qiagen has submitted a PMA with the FDA for its Therascreen EGFR RGQ PCR Kit, which gauges whether a patient's tumor is EGFR-mutation positive.

As part of the NDA for afatinib, Boehringer submitted data from the LUX-Lung clinical trial program, including LUX-Lung 3. Data from this trial showed that advanced adenocarcinoma patients with EGFR mutations treated with afatinib lived for 11.1 months without their tumor growing compared to 6.9 months for patients treated with best-in-class chemotherapy agents containing cisplatin and pemetrexed. LUX-Lung 3 represents the largest Phase III trial conducted to date in first-line EGFR mutation-positive, locally advanced, or metastatic NSCLC patients (PGx Reporter 6/6/2012).

For the companion EGFR mutation test, Qiagen submitted to the FDA analytical studies including "limit of the blank, limit of detection, accuracy, interfering substances, repeatability and reproducibility," a Qiagen spokesperson told PGx Reporter. The firm also submitted data from LUX-Lung 3, in which approximately
90 percent of patients had the most common EGFR mutations, Del19 and L858R.

The Therascreen EGFR RGQ PCR Kit includes seven mutation assays that gauge 29 mutations. There are four singleplex assays that assess T790M, L858R, L861Q and S768I mutations, and three multiplex assays that gauge a number of deletions, insertions, and G719X mutations.

"The automated calling software will report whether a mutation has been detected or not detected in each mutation assay," the Qiagen spokesperson explained. "For the multiplex mutation assays, when a mutation is detected, the kit reports a mutation but does not distinguish which mutation in the multiplex assay has been detected."

EGFR mutations occur in 10 percent to 15 percent of the approximately 200,000 people diagnosed with advanced NSCLC each year in the US. However, Boehringer estimates that only 50 percent of NSCLC patients are being tested for EGFR mutations. Even then, the company has noted that even when patients receive testing, they don't receive test results early enough to influence a personalized treatment strategy.

To ensure that the patients who can benefit from afatinib are identified, Boehringer launched the "Let's Test" campaign last year to educate healthcare providers about biomarker testing, specifically EGFR and ALK mutations testing, in NSCLC patients. The effort is aimed at encouraging doctors to collect sufficient amounts of tissue from NSCLC patients and test them for these mutations early so that they can choose a treatment strategy that is individualized and has a positive impact on patient outcomes (PGx Reporter 10/24/2012).

Boehringer told PGx Reporter that to date the website for the Let's Test campaign has had more than 17,000 visitors. The education effort appears to have paid off. The company cited market research data that found that in the fourth quarter of 2012 EGFR mutation testing in advanced non-squamous NSCLC patients was being performed for approximately 70 percent of the patient population — up from around 40 percent in the last quarter of 2011.

"Unfortunately there are still thousands of patients with advanced NSCLC that never have their mutations status determined, so education is still important," a Boehringer spokesperson said. "Testing rates are higher in academic and comprehensive cancer centers than they are in many communities, but there is an opportunity to make improvements in both testing rates and providing test results more quickly."

Tarceva

Astellas' supplemental NDA for Tarceva is seeking approval for the drug as a first-line treatment for locally advanced or metastatic NSCLC in patient whose tumors have EGFR mutations. The drug is already approved as a treatment for later stages of advanced NSCLC. Roche, meanwhile, is seeking premarket approval for the companion test, the Cobas EGFR Mutation Test.

As part of the sNDA, Astellas submitted data from the randomized, prospective, Phase III EURTAC trial, comparing first-line use of Tarceva against platinum-based chemotherapy in 174 patients with EGFR activating mutation-positive advanced NSCLC. The European Commission approved the drug in 2011 in NSCLC patients with EGFR mutations using data from the same study (PGx Reporter 9/7/2011).

In EURTAC, Tarceva nearly doubled median progression-free survival compared to chemotherapy — 9.7 months compared to 5.2 months. Patients in the Tarceva arm also had a 63 percent reduced risk of their cancer progressing compared to those in the chemotherapy arm. The study was stopped early after it met its primary endpoint (PGx Reporter 6/8/2011).