What Is Erlotinib (Tarceva)? FDA Approval, Licensing and Reimbursement in Turkey
In this article
- FDA Approval: Yes, it received FDA approval in November 2004.
- Brand Name: Tarceva
- Active Ingredient: Erlotinib hydrochloride
- Route of Administration: Oral tablet (taken 1 time daily, on an empty stomach)
- Class: Small-molecule tyrosine kinase inhibitor (TKI)
- Category: Targeted therapy, EGFR inhibitor
- Manufacturer: Initially OSI Pharmaceuticals and Genentech/Roche; currently marketed by Roche/Genentech
- Distribution in Turkey: Distributed in Turkey by Roche İlaç
- Approved Cancers: Non-Small Cell Lung Cancer (NSCLC): Particularly in patients with EGFR mutations; Pancreatic Cancer: In combination with gemcitabine (approved in the United States and some regions; use in Turkey is limited)
What Is Erlotinib? How Does It Work?
The small-molecule active ingredient erlotinib is designed to bind to the epidermal growth factor receptor(EGFR) on the surface of lung cancer cells. When the drug binds to the receptor, erlotinib blocks the signal telling cancer cells to grow and divide. The EGFR receptor is normally also present on the surface of healthy cells, but may be found in very high quantities on cancer cells or in a mutated form. To determine whether there is an EGFR mutation that will respond to erlotinib, before starting erlotinib, genetic testing is performed.
In non-small cell lung cancer, EGFR overexpression is seen in 70% of patients. However, it is the presence of an EGFR mutation that determines treatment response. Approximately 1 in every 7 patients with non-small cell lung cancer has this mutation.
- Related Topic: What Is an EGFR Mutation? How Is EGFR Testing Performed in Lung Cancer?
Erlotinib is the name of the active ingredient; it is available on the market under the names Tarceva, Ertinob and Tarsinib.
FDA (United States Food and Drug Administration) Approval History
18 November 2004: Erlotinib first received FDA approval for metastatic or locally advanced non-small cell lung cancer (NSCLC). The initial approval was as monotherapy for patients who had not responded to at least one previous chemotherapy regimen.
2 November 2005: FDA approval was granted for treating advanced, unresectable or metastatic pancreatic cancer in combination with gelatin.
18 April 2010: Erlotinib was approved as maintenance treatment in patients with NSCLC whose disease had not progressed following platinum-based first-line chemotherapy.
14 May 2013: Erlotinib received FDA approval as first-line treatment for patients with metastatic NSCLC carrying an EGFR ex13 19 deletion or ex21 L858R mutation. The accompanying cobas EGFR Mutation Test (Roche) diagnostic test was also approved for this classification.
18 October 2016: With an FDA label update, erlotinib use was restricted to patients with EGFR-mutated (exon 19 or exon 21 L858R) NSCLC (in maintenance and second/subsequent lines of treatment).
Licensing in Turkey
In Turkey, erlotinib (for example, under the brand “Ertinob”) has a formulation licensed by Nobel İlaç, with its first licensing date stated as 15 September 2017.
SGK Reimbursement Status
For advanced/metastatic non-small cell lung cancer (NSCLC) that is EGFR mutation-positive (Exon 19 deletion or L858R mutation), it is covered by SGK as first-line or subsequent-line treatment. It is available on the market as Tarceva, Ertinob, Tarsınıb, Etınıb, Sevastra, Tartada, Bitinol, Lungerlo, Tarcetin and Ertivec.
March 2026 Price: Tarceva 150 mg tablet costs 33.967,31 TL, Tarceva 25 mg 30 tablets costs 9.433,16 TL, and Tarceva 100 mg 30 tablets costs 27.266,67 TL.
Cost of One “Cycle” (1 Month) of Erlotinib
erlotinib daily as an oral medicine, so in practice the cost is usually assessed over 1 month (30 tablets) .
| Daily Dose | 30-Day Requirement | Packaging / Purchase | Approximate Cost for 1 Month | Note |
|---|---|---|---|---|
| 150 mg/day (standard starting dose) | 30×150 mg | Tarceva 150 mg (30 tablets) ×1 | 33.967,31 TL | 1 box is sufficient. |
| 125 mg/day | 30×(100+25) mg | 100 mg (30 tablets) ×1 + 25 mg (30 tablets) ×1 | 36.699,83 TL | Practical “100+25” combination. |
| 100 mg/day | 30×100 mg | Tarceva 100 mg (30 tablets) ×1 | 27.266,67 TL | 1 box is sufficient. |
| 75 mg/day | 30×(25+25+25) mg | 25 mg (30 tablets) ×3 | 28.299,48 TL | 3 boxes of 25 mg tablets are needed. |
| 50 mg/day | 30×(25+25) mg | 25 mg (30 tablets) ×2 | 18.866,32 TL | 2 boxes of 25 mg tablets are needed. |
| 25 mg/day | 30×25 mg | 25 mg (30 tablets) ×1 | 9.433,16 TL | 1 box is sufficient. |
Mechanism of Action
- It binds to the tyrosine kinase region of the Epidermal Growth Factor Receptor (EGFR), inhibiting phosphorylation.
- This blockade stops cell proliferation, invasion and angiogenesis, and leads to apoptosis and suppression of growth in tumor cells.
Pharmacokinetics
Absorption
- When taken orally, its bioavailability is approximately 60%.
- Absorption increases when taken with food (a particularly fatty meal may increase bioavailability up to 2 times).
- It reaches maximum plasma concentration within 3–4 hours.
Distribution
- It binds strongly to plasma proteins (93–95%, particularly albumin and α-1 acid glycoprotein).
- It has a large volume of distribution → it penetrates tissues well, particularly lung tumor tissue.
Metabolism
- It is metabolized primarily by CYP3A4 in the liver.
- CYP1A2 and CYP1A1 also play a lesser role.
- It has no active metabolite; most metabolites are inactive.
Elimination
- Erlotinib and its metabolites are eliminated mainly through bile/feces (over 80%).
- Urinary elimination is low (<10%).
- The average elimination half-life is 36 hours; once-daily administration is suitable.
Route of Administration, Dose and Schedule
Starting dose: 150 mg oral tablet once daily by mouth. Erlotinib is a pill-form medicine that can be used at home, classified as molecularly targeted smart cancer therapy . Erlotinib is taken continuously every day for as long as the tumor continues to respond to treatment or until unacceptable side effects occur.
Side Effects
The side effects most frequently reported with erlotinib in clinical studies are listed below. Side effects sometimes have percentage ranges because they vary between clinical settings (for example, 76 - 80%);
- Rash (76 - 80%)
- Fatigue (57 - 79%)
- Diarrhea (57%)
- Nausea (40%)
- Infection (34%)
- Decreased appetite (31 - 69%)
- Eye infection (28%)
- Vomiting (25%)
- Mouth sores (19%)
- Hair loss or thinning; it does not cause complete hair loss. (14%)
- Anemia [low red blood cells] (12%)
- Joint pain (11%)
- Pain in the fingertips (9%)
- Fluid loss (7%)
- Liver damage (6%)
- Lung infection (1-3%)
Approximately 6% of patients discontinue erlotinib treatment because of unacceptable side effects.
How Often Is Monitoring Needed?
Blood tests are recommended before treatment. The required blood tests are a complete blood count (hemogram) and a comprehensive metabolic panel (biochemistry). Other blood tests may be added at the physician’s recommendation. Your physician will decide how often these blood tests will be performed.
How Often Is Imaging (Radiological Assessment) Needed?
Imaging may be performed before treatment, immediately after treatment ends and during routine follow-up. Imaging includes computed tomography (CT) scans, magnetic resonance imaging (MRI), and positron emission tomography (PET/CT). You may have an eye examination before starting treatment and again 4 to 8 weeks after starting treatment to check for any eye infection.
How Do Blood Test or Imaging Results Affect Treatment?
Depending on the results, your doctor may continue erlotinib as planned, change its dose or change the treatment.
Things to Consider During Erlotinib Treatment
- It is extremely important to tell your doctor if you are actively smoking while taking erlotinib. Smoking can cause erlotinib to be broken down faster than normal, reducing its effectiveness. In general, patients who continue smoking and experience no side effects increase their doses every 2 weeks up to a maximum of 300 mg per day. If you decide to stop smoking after your dose has been increased, tell your doctor immediately.
- Skin rash commonly develops during erlotinib use. However, the development of skin rashes may be related to the disease rather than being a side effect of erlotinib. Mild skin rashes can be treated with simple lotions or topical steroids. More serious rashes may be treated with oral or topical antibiotics or oral steroids prescribed by your doctor. Tell your doctor about any skin reactions you have.
- Erlotinib becomes less effective when taken with medicines for heartburn or medicines that reduce stomach acid. When these medicines are needed, talk to your doctor or pharmacist about how to take these two medicines.
- If you are going to any hospital or emergency department, make sure to bring your erlotinib medicine with you. Many hospitals cannot supply this medicine.
- Erlotinib has numerous drug-drug interactions. Your oncology pharmacist should always review your medicine list to ensure that drug interactions are appropriately prevented or managed.
Drug Label Information
Erlotinib (Tarceva, Ertinob, Tarsinib)
- Erlotinib is an oral tablet available in 25 mg, 100 mg and 150 mg strengths.
- Erlotinib should be taken on an empty stomach, at least 1 hour before food or two hours after a meal. Food increases absorption of the drug, so taking it on an empty stomach is best to avoid increased side effects. Erlotinib may be taken at any time of day, as long as it is taken at the same time every day.
- If you miss a dose, take it as soon as you remember. On the following day, take your regular dose as scheduled. Do not double your dose to make up for the missed dose.
- Erlotinib should be stored at room temperature in a cool, dry place.
- Dosage adjustments may be needed for smoking, drug interactions and serious side effects.
- It may interact with medicines for heartburn or medicines that reduce stomach acid. Short-acting antacids (for example, Rennie) or H2 antagonists (Ranitab, Ulcuran) may be used instead of proton pump inhibitors. These medicines should be taken at least 2 hours before erlotinib.
- It may interact with certain antifungal and seizure medicines. Ask your doctor or pharmacist to review your medicines for possible interactions.
- Grapefruit and grapefruit juice may interact with it and increase blood levels of erlotinib. This may increase your risk of side effects. Avoid grapefruit and anything containing grapefruit juice during treatment.
- Avoid St. John’s wort and smoking because they lower blood levels of erlotinib and may reduce its effectiveness
- Avoid during pregnancy. If you think you may be pregnant, contact your doctor immediately.
Sources
Erlotinib in previously treated non–small-cell lung cancer.
New Engl J Med. 2005.
2. Rosell R, Carcereny E, Gervais R, et al.
Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial.
Lancet Oncol. 2012.
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