Erlotinib

Erlotinib is an anticancer medicine marketed under the name Tarceva ®.

Indications

For what it uses

The use of erlotinib is indicated for the treatment of:

Advanced non-small cell lung cancer;
Metastatic stage pancreatic carcinoma, usually in combination with gemcitabine. Erlotinib - Chemical Structure

Warnings

Your doctor may decide to stop treatment with erlotinib if the following symptoms appear:

Sudden difficulty in breathing associated with cough and fever;
Severe and persistent diarrhea;
Nausea, loss of appetite or vomiting;
Acute redness and eye pain, increased tearing, blurred vision and / or sensitivity to light;
Intense abdomen pain;
Severe skin reactions, such as - for example - blistering or flaking.

Erlotinib treatment is not recommended in patients with liver and / or kidney disease.

In patients with glucuronidation disorders - such as Gilbert's syndrome (a disorder of bilirubin metabolism) - erlotinib should be used with caution.

No smoking is required during erlotinib therapy, as smoking is able to decrease plasma concentration and - consequently - erlotinib efficacy.

Erlotinib therapy is not recommended in children and adolescents.

Erlotinib should not be taken with food.

Interactions

Concomitant administration of erlotinib and anticoagulants - such as, for example, warfarin - may increase the risk of bleeding and bleeding.

The concomitant intake of erlotinib and statins (drugs used to decrease blood cholesterol concentration) can cause an increased risk of statin-related muscle damage. Such damage - in some cases - can lead to rhabdomyolysis (rupture of skeletal muscle cells and release into the bloodstream of substances contained in the musculature), with consequent renal damage.

The combination of erlotinib and capecitabine (an anticancer agent) may cause an increase in the plasma concentration of erlotinib itself.

It would be good to avoid the concomitant use of erlotinib and the following medicines, as there may be a decrease in the therapeutic efficacy of erlotinib or an increase in its side effects:

Antifungal drugs, such as ketoconazole ;
Protease-inhibiting antiviral drugs, such as - for example - ritonavir ;
Erythromycin and clarithromycin, antibiotic drugs;
Phenytoin and carbamazepine, drugs used to treat epilepsy;
Barbiturates ;
Rifampicin, an antibiotic used in the treatment of tuberculosis;
Ciprofloxacin, a quinolone antibiotic;
Omeprazole and ranitidine, drugs used to reduce acid secretion of the stomach;
St. John's wort (or St. John's wort), a plant that has antidepressant properties.

Side effects

Erlotinib can induce various types of side effects although not all patients experience them. The type of side effects and the intensity with which they occur varies from person to person, depending on the sensitivity that each patient has towards the drug.

The following are the main side effects that may occur following treatment with erlotinib.

Gastrointestinal disorders

Treatment with erlotinib may cause nausea, vomiting and diarrhea.

If they are mild, these symptoms can be treated with anti-emetic and anti-diarrheal drugs.

On the contrary, if these symptoms occur in a severe manner, it is necessary to immediately contact the doctor who could decide to stop the therapy and to admit the patient to the hospital. Severe and persistent diarrhea can lead to a reduction in the blood concentration of potassium (hypokalemia) and renal failure, especially in patients who are simultaneously treated with other chemotherapy drugs.

In addition, the drug can cause stomach pain, flatulence, indigestion, bleeding from the stomach or intestines and intestinal perforation.

Respiratory disorders

Treatment with erlotinib may cause breathing difficulties associated with cough and fever. These may be signs of the onset of interstitial lung disease. This disease can also have fatal outcomes.

Eye disorders

Treatment with erlotinib may cause inflammation of the colored part of the eye, conjunctivitis, keratoconjunctivitis (simultaneous inflammation of the cornea and conjunctiva) and keratitis (inflammation of the cornea). Furthermore, cases of corneal ulceration and perforation have been reported.

Hepatobiliary disorders

Treatment with erlotinib may cause changes in liver function and liver failure.

Skin and subcutaneous tissue disorders

Treatment with erlotinib may cause skin rashes that may occur or worsen in areas exposed to sunlight. Therefore, it is recommended to protect the skin with clothing and sunscreens.

Erlotinib can also cause alopecia, acne, dry skin, skin fissures, inflammatory reactions around the nails, infection of the hair follicles and Stevens-Johnson syndrome (a more severe variant of polymorphic erythema).

Nervous system disorders

Erlotinib can cause headaches, fatigue, changes in skin sensitivity, numbness in the extremities and can induce depression.

Other side effects

Other types of side effects that may occur during erlotinib therapy are:

Infections;
Loss of appetite and body weight;
Irritations of the mouth;
Temperature;
Chills;
Nose bleeding;
Changes in eyelashes and eyebrows;
Excessive hair on the face and body;
Fragility of nails that can also come off;
Hand-foot syndrome, a syndrome characterized by redness and / or pain in the palm of the hands and the soles of the feet.

Overdose

In the event of an overdose with erlotinib, an exacerbation of side effects may occur. If you suspect you have taken an overdose of medication, you should contact a doctor or the nearest hospital immediately.

Action mechanism

Erlotinib exerts its antitumor action by inhibiting the epidermal growth factor receptor (EGFR).

EGFR is involved in the growth, proliferation, diffusion and metastasis processes of cancer cells. Therefore, by inhibiting this receptor, erlotinib is able to stop the proliferation and spread of the tumor mass.

Mode of Use - Posology

Erlotinib is available for oral administration as tablets. The tablet should be taken one hour before or two hours after food intake.

The dosage of erlotinib must be established by the doctor according to the pathology to be treated and the patient's condition.

The dosages of erlotinib usually used are given below.

Advanced non-small cell lung cancer

For this type of cancer, the usual erlotinib dose is 150 mg per day. Depending on the patient's response to the therapy, the doctor may decide to change the drug dose.

Metastatic carcinoma of the pancreas

In this case, the dose of erlotinib usually given is 100 mg of drug per day. Depending on how the patient responds to therapy, the doctor will decide whether or not to increase the amount of drug administered.

Pregnancy and breastfeeding

The use of erlotinib by pregnant women should be avoided.

Furthermore, adequate precautions must be taken in order to prevent the onset of pregnancies, both during treatment with the drug and for a period of at least two weeks from the end of the same.

Breast-feeding mothers should not take erlotinib.