Tarceva

Generic Name: Erlotinib hydrochloride
Product Name: Tarceva

Indication: What Tarceva is used for

Tarceva is a medication used in cancer treatment. It may be used to treat people who have advanced non-small cell lung cancer (NSCLC) or pancreatic cancer.

For people with lung cancer, Tarceva is used as a second-line therapy, and is only used when the cancer does not improve well enough with the first treatment option.

When used to treat pancreatic cancer, Tarceva is used in combination with gemcitabine, another anti-cancer medication.

Action: How Tarceva works

The active ingredient in Tarceva, erlotinib, has been shown to inhibit the growth of cancerous tumours and cause cancerous cells to die. It does this by altering the action of a protein called human epidermal growth factor receptor (HER or EGFR). When it functions normally, HER helps cancer cells to multiply. Altering the action of HER can prevent the growth of cancer cells.

Dose advice: How to use Tarceva

Dose information

The recommended dose of Tarceva depends on whether it is used to treat lung or pancreatic cancer. It should only be taken as instructed by your doctor. If you take more Tarceva than the doctor has prescribed, you should contact the Poisons Information Centre immediately, even if there are no immediate signs of illness. Tarceva should not be given to people for whom it has not been prescribed. If some one else takes your medication, the Poisons Information Centre should be contacted immediately.

Tarceva tablets should be swallowed whole. They should not be crushed or chewed. The medicine should be taken one hour before or two hours after eating. It should not be taken with food.

If you forget to take a dose of Tarceva, skip that dose and take the medication again when it is next due. Make sure you tell your doctor if you skip a dose or are unable to take Tarceva according to the schedule prescribed. Your doctor will need to consider this information when determining whether or not the treatment is effective or the dose requires adjustment. It’s also important to tell your doctor about any other medications you use (including herbal remedies and supplements), as these may influence the effectiveness of Tarceva.

Check the expiry date before using Tarceva tablets. Do not use Tarceva if the packaging is damaged.

Non-small cell lung carcinoma (NSCLC)

The initial recommended dose for the treatment of NSCLC is 150 mg. The dose should be taken one hour before or two hours after eating. Your doctor may adjust the dose as treatment progresses, or to account for the effects of other medications you are taking. The dose may be reduced if liver problems develop.

Pancreatic cancer

When used to treat pancreatic cancer, Tarceva is used in combination with another anti-cancer medication called gemcitabine. The recommended dose is 100 mg of Tarceva, one hour before or two hours after food. Your doctor may adjust the dose as treatment progresses, or to account for the effects of other medications you are taking. The dose may be reduced if liver problems develop.

If you have any queries about the correct way to use Tarceva, please ask your doctor.

Contraindications

Tarceva should not be used under certain conditions. Tell your doctor if you have:

Allergies, especially if you know you are allergic to Tarceva or one of its ingredients;
Lactose intolerance.

Precautions

Special care needs to be taken when using Tarceva under certain conditions. Tell your doctor if you have (or develop in the course of treatment):

Breathing difficulties: Including breathlessness, cough or fever. You may be at increased risk of experiencing a severe breathing problem whilst undergoing Tarceva therapy. Your doctor may therefore need to monitor you more closely;
Diarrhoea: You may require medicine to reduce diarrhoea, or treatment for dehydration (a common side effect of diarrhoea);
Kidney problems: The risks of Tarceva treatment are greater in patients with kidney disorders, and your doctor may need to take additional measures to reduce associated risks. If you develop kidney problems in the course of treatment, it may be necessary to stop treatment;
Liver problems: The risks associated with Tarceva treatment are greater for people with liver problems. Your doctor may need to monitor your liver function more frequently;
Gastrointestinal problems: Including peptic ulcer or diverticular disease. These increase the risk of gastrointestinal perforation (a hole in the stomach or intestines allowing the content of the stomach to flow out), a potentially fatal consequence of Tarceva therapy;
Skin disorders: Including rashes. These have the potential to develop into serious and potentially fatal conditions, and adjustments to the treatment may be needed to prevent them;
Eye problems: Including pain, abnormal eyelash growth, dry eyes or irritation. These may lead to corneal perforation and ulceration, and adjustments to the treatment may be needed to prevent them;
Taking other medications;
Smoking.

Drug interactions

Many medications interact with and alter the action of Tarceva. For example, they might increase or decrease the amount of Tarceva absorbed by the body. Therefore, it is important to tell your doctor about all other medicines you use, including over-the-counter medicines or herbal remedies. Drugs that interact with Tarceva include:

pH-altering drugs: Drugs used to treat dyspepsia or heartburn alter the pH (acidity) of the upper gastrointestinal tract. The rate at which Tarceva is absorbed depends on the body’s pH, so heartburn treatments can affect the absorption of Tarceva. Histamine 2 receptor agonists are the recommended heartburn treatment for people receiving Tarceva therapy;
Drugs metabolised in the liver similar to Tarceva may either increase or decrease the metabolism of Tarceva. These include:
- Ketoconazole;
- Ciprofloxacin;
- Atazanavir;
- Clarithromycin;
- Erythromycin;
- Indinavir;
- Itraconazole;
- Nefazodone;
- Nelfinavir;
- Ritonavir;
- Saquinavir;
- Telithromycin;
- Troleandomycin;
- Voriconazole;
- Rifampicin;
- Rifabutin;
- Rifapentine;
- Phenytoin;
- Carbamazepine;
- Phenobarbitone;
- St John’s wort.
Smoking: Smoking reduces the absorption of Tarceva.

Some medications increases the risk of gastrointestinal perforation when used with Tarceva. These include:

Anti-angiogenics (medications which promote the growth of new blood vessels);
Corticosteroids;
Non-steroidal anti-inflammatory drugs (NSAIDs); and
Taxane-based chemotherapy drugs.

Anticoagulant medications used in combination with Tarceva increase the risk of abnormal bleeding. Your doctor may need to monitor your blood clotting if you are taking these two medications together.

Statins (medicines used to control cholesterol levels) may increase the risk of myopathy (muscle weakness) if administered in combination with Tarceva.

Pregnancy

Tarceva is a Pregnancy Category C medication and should not be used by pregnant women. No studies have been done in humans but animal studies indicate that Tarceva has the potential to harm the foetus of a pregnant woman who uses the medication. Growth of the foetus may be restricted, it may develop lung abnormalities, and the woman has an increased risk of miscarriage. Tarceva is only prescribed for pregnant women when the potential benefits to the woman outweigh the risks to the foetus. Women of reproductive age should use contraception if they are sexually active while undergoing treatment.

Breastfeeding

Studies have not been conducted to determine the safety of Tarceva use whilst breastfeeding. It is not known if the medicine is passed on to the baby via the mother’s milk. Breastfeeding women should not use Tarceva.

Children

There are no data regarding the efficacy or safety of Tarceva for use in children. Tarceva should not be used by people less than 18 years of age.

Schedule of Tarceva

Tarceva is a Schedule 4 medication.¹

Common side effects of Tarceva

All medicines have side effects. Most commonly the side effects are minor; however, some can be more serious. Usually the benefits of taking a medication outweigh the associated side effects. Your doctor would have considered these side effects before starting you on Tarceva.

The side effects of Tarceva differ depending on the condition it is used to treat: NSCLC or pancreatic cancer.

Side effects of Tarceva therapy for non-small cell lung cancer

Side effects are common with Tarceva therapy for NSCLC, and 99% of patients experience one or more side effects. The majority (60%) of events are minor, while 22% of side effects experienced are severe.

Very common side effects

Very common side effects are those that occur in more than 10% of people given Tarceva. When Tarceva is used to treat lung cancer, these include:

Rash (75%);
Pruritis (skin irritation) (13%);
Dry skin (12%);
Diarrhoea (54%);
Nausea (33%);
Vomiting (23%);
Stomatitis (inflammation of the mouth) (17%);
Abdominal pain (11%);
Fatigue (52%);
Rigors (intense shivering attacks) (12%);
Infection, including severe pneumonia, sepsis and cellulitis (31%);
Depression (19%);
Cough (16%);
Headache (15%);
Neuropathy (nerve degeneration, leading to loss of function) (13%).

Common side effects

Common side effects are those that occur in 1–10% of people given Tarceva. For lung cancer treatment, side effects which occur commonly include:

Severe rash (9%);
Severe diarrhoea (6%);
Alopecia (hair loss);
Liver function test abnormalities (indicating the liver is not functioning properly);
Epistaxis (nose bleed);
Skin fissures (cracked skin);
Paronychia (abscess of the fingernail).

Uncommon side effects

Side effects that occur in less than 1% of people given Tarceva are considered uncommon. People do not necessarily experience any of these side effects, so do not become alarmed by this list:

Interstitial lung disease (a chronic lung disorder which results in difficulty breathing);
Gastrointestinal perforations (tears in the stomach or intestines which allow the stomach contents to leak out);
Abnormal eyelash growth, including in-growing, excessive growth and thickening;
Hirsutism (excessive hair growth);
Hyperpigmentation (skin discolouration).

Rare side effects

Rare side effects are those that occur in 0.01–0.1% of people given Tarceva. These include:

Liver failure;
Hepatorenal syndrome (kidney failure in an individual with existing liver disease).

Very rare side effects

Very rare side effects are those that occur in less than 0.01% of people given Tarceva. These include:

Corneal perforation (an injury to the cornea of the eye which affects vision);
Corneal ulceration;
Stevens-Johnson syndrome/toxic epidermal necrolysis (a potentially fatal condition characterised by inflammation and blistering of the skin).

If you experience any of the listed side effects, or any other symptoms that appear abnormal or unusual, please tell your doctor.

Side effects of Tarceva therapy for pancreatic cancer

When used to treat pancreatic cancer, Tarceva is used in combination with another anti-cancer medicine called gemcitabine. Side effects are also common when Tarceva is used to treat pancreatic cancer, and 99% of patients experience one or more adverse event. The majority (60%) of side effects are minor, while 22% of side effects experienced are classified as severe.

Very common side effects

Very common side effects are those that occur in more than 10% of people given Tarceva. When Tarceva is used to treat pancreatic cancer, these include:

Rash (69%);
Alopecia (hair loss) (14%);
Diarrhoea (48%);
Stomatitis (inflammation of the mouth) (22%);
Dyspepsia (indigestion) (17%);
Flatulence (excessive stomach gas) (13%);
Weight reduction (39%);
Pyrexia (fever) (36%);
Fatigue (73%);
Anorexia (loss of appetite) (52%);
Dyspnoea (breathing difficulty) (41%);
Cough (33%);
Infection (24%).

Common side effects

Common side effects are those that occur in 1–10% of people given Tarceva. For pancreatic cancer treatment, side effects which occur commonly include:

Heart attack/myocardial ischaemia (reduced blood flow to the heart) (2.3%);
Other acute events affecting the blood vessels to the brain (2.3%);
Liver function test abnormalities (indicating problems with liver function);
Epistaxis (nose bleed);
Skin fissures (cracked skin);
Paronychia (abscess of the fingernails).

Uncommon side effects

Side effects that occur in less than 1% of people given Tarceva are considered uncommon. People do not necessarily experience any of these side effects, so do not become alarmed by this list:

Interstitial lung disease (a chronic lung disorder which results in difficulty breathing);
Gastrointestinal perforations (tears in the stomach or intestines which allow the stomach contents to leak out);
Abnormal eyelash growth, including in-growing, excessive growth and thickening;
Hirsutism (excessive hair growth);
Hyperpigmentation (skin discolouration).

Rare side effects

Rare side effects are those that occur in 0.01–0.1% of people given Tarceva. These include:

Liver failure;
Hepatorenal syndrome (kidney failure in an individual with existing liver disease).

Very rare side effects

Very rare side effects are those that occur in less than 0.01% of people given Tarceva. These include:

Corneal perforation (an injury to the cornea of the eye which affects vision);
Corneal ulceration;
Stevens-Johnson syndrome/toxic epidermal necrolysis (a potentially fatal condition characterised by inflammation and blistering of the skin).

If you experience any of the listed side effects, or any other symptoms that appear abnormal or unusual, please tell your doctor.

For further information talk to your doctor.

References

Tarceva [online]. St Leonards, NSW: MIMS Online; 12 February 2010 [cited 5 October 2010]. Available from: URL link
Consumer Medical Information: Tarceva. Dee Why, NSW: Roche Products Pty Ltd; 15 March 2010.
Product Information: Tarceva. Dee Why, NSW: Roche Products Pty Ltd; 15 October 2010.