Tarceva (erlotinib) is a tyrosine kinase inhibitor approved by the U.S. Food and Drug Administration (FDA) for the treatment of certain types of non-small cell lung cancer (NSCLC) that have spread to nearby tissues or to other parts of the body. The drug is used in patients who already have been treated, ineffectively, with at least one other chemotherapy agent.

Tarceva works in NSCLC patients whose cancer cells have alterations in specific receptors called epidermal growth factor receptors (EGFRs) found on their surface. These alterations cause the cells to grow and multiply out of control.

EGFRs can be activated by several molecules in our bodies, and upon their activation, molecular signals trigger the expression of new portions of the genetic material that, ultimately, inhibit cellular death and lead to cellular proliferation, migration, and adhesion.

It can affect both healthy cells and cancer cells, and it is not known whether the drug is safe and effective in EGFR mutations other than those included in the FDA-approved prescribing information.

How Tarceva works

Tarceva still allows for the bond between ECFRs and their ligands to occur, but blocks the activation of the receptor by inhibiting its tyrosine kinase activity that initiates the molecular signal that triggers cancer cell proliferation.

Tarceva in clinical trials

The efficacy as an initial therapy was studied in a multicenter, open-label, randomized, Phase 3 trial (NCT01342965) that enrolled 174 patients with metastatic NSCLC whose tumors tested positive for certain EGFR mutations. During this trial, the efficacy of Tarceva was compared to that of conventional chemotherapy.

Results showed that patients who took Tarceva had a 66 percent lower risk of cancer progression or death compared to those who received conventional chemotherapy. Patients who received Tarceva had a median overall survival time of 22.9 months compared to 19.5 months for those who received conventional chemotherapy. However, this difference was not enough to conclude that the median overall survival time was better with Tarceva than with chemotherapy, in a statistical sense. Tumors shrank or disappeared for 65 percent of patients who received Tarceva and 16 percent of patients who received chemotherapy.

The latest FDA approval determined that Tarceva was safe and effective only in patients with metastatic NSCLC tumors, with EGFR-activating mutations, based on the results of a double-blind, placebo-controlled, Phase 4 trial (NCT01230710). In this trial, it was administered to 643 patients who had not experienced disease progression during four cycles of platinum-based first-line chemotherapy. Patients with metastatic NSCLC tumors harboring EGFR-activating mutations were excluded from this study. Participants were randomized to either receive Tarceva or placebo by mouth once daily until the disease progressed or the level of toxicity became unacceptable.

Results demonstrated that survival following treatment with Tarceva was not better than placebo administered as maintenance in patients with metastatic NSCLC tumors not harboring EGFR-activating mutations. No difference in progression-free survival between the Tarceva arm and the placebo arm was observed.

There are several trials currently recruiting participants to study the safety and effectiveness of Tarceva in conjugation with other anti-cancer drugs, such as BGB324 (NCT02424617),  INCB028060 (NCT01911507NCT02468661), Tecentriq (atezolizumab – NCT02013219), and Avastin (bevacizumab – NCT03126799).

Other information

The most common side effects of are diarrhea, weakness, rash, cough, shortness of breath, and loss of appetite.

Tarceva comes as a tablet to be taken by mouth once a day on an empty stomach (at least one hour before or two hours after eating a meal or a snack). Taking it with food may increase the risk of side effects.

Tarceva also is used in combination with another medication — Gemzar (gemcitabine) — to treat pancreatic cancer that has spread to nearby tissues or to other parts of the body and cannot be treated with surgery.

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