Therapeutic Group : Tyrosine Kinase Inhibitor (Oncology)
Erlotinib is a tyrosine kinase inhibitor which reversibly inhibits the kinase activity of EGFR(Epidermal Growth Factor Receptor). It prevents autophosphorylation of tyrosine residues associated with the receptor and thereby inhibiting further downstream signaling. The absorption of this drug is 60%. Metabolism occurs in liver (CYP mediated, mainly CYP3A4 and a lesser extent by CYP1A2). This drug is eliminated by feces (83%) and urine (8%). It has a half-life (t1/2) of 36.2 hours.
Erlotinib Hydrochloride Presentation:
– Ertinib is indicated for the first-line treatment of patients with metastatic NSCLC.
– Ertinib is indicated for the maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum-based first-line chemotherapy.
– It is also indicated for the treatment of patients with locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
– Ertinib is not recommended for use in combination with platinum-based chemotherapy.Pancreatic cancer:
Ertinib in combination with Gemcitabine is indicated for the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer.
– Ertinib 150 mg once daily taken on an empty stomach.Pancreatic Cancer:
– Ertinib 100 mg once daily taken on an empty stomach in combination with Gemcitabine.
– Ertinib should be taken at least one hour before or two hours after the ingestion of food.
Pregnancy: Pregnancy category D. Erlotinib can cause fetal harm. Women should be advised to avoid becoming pregnant while receiving treatment with Erlotinib.
Nursing mothers: It is not known whether Erlotinib is excreted into human milk or not. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric use: The safety and efficacy of Erlotinib has not been established in pediatric cases.
Geriatric Use: The safety and efficacy of Erlotinib was similar in older and younger patients.
Hepatic Impairment: Hepatotoxicity occurs with or without hepatic impairment, including hepatic failure and hepatorenal syndrome; monitor periodic liver testing. Erlotinib should be withheld or discontinued for severe or worsening liver tests.
Renal Impairment: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
Gastric: Patients receiving concomitant anti-angiogenic agents, corticosteroids, NSAIDs, or taxane-based chemotherapy, or who have prior history of peptic ulceration or diverticular disease may be at increased risk of gastrointestinal perforation (0.2-0.4%).
Patients taking anticoagulants: Severe and fatal hemorrhage can occur when Erlotinib and warfarin are administered concurrently. Regularly monitor prothrombin time and INR during Erlotinib treatment in patients taking warfarin or other coumarin-derivative anticoagulants.
CYP3A4 inhibitors: CYP3A4 inhibitors (itraconazole, ketoconazole, voriconazole, atazanavir, indinavir, nelfinavir, ritonavir, saquinavir, clarithromycin, telithromycin, troleandomycin (TAO), nefazodone, or grapefruit or grapefruit juice) or with an inhibitor of both CYP3A4 and CYP1A2 (ciprofloxacin) increases the AUC of Erlotinib. Avoid concomitant use if possible. Reduce Erlotinib use by 50 mg decrements.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with ranitidine 300 mg decreased Erlotinib AUC by 33%. Avoid concomitant use of Erlotinib with proton pump inhibitors if possible. Separation of doses may not eliminate the interaction. If treatment with an H2-receptor antagonist such as ranitidine is required, Erlotinib must be taken 10 hours after the H2-receptor antagonist dosing and at least 2 hours before the next dose of the H2-receptor antagonist. Although the effect of antacids on Erlotinib pharmacokinetics has not been evaluated, the antacid dose and the Erlotinib dose should be separated by several hours, if an antacid is necessary.
Ertinib 150 Tablet: Each box contains 10 tablets in Alu-Alu blister pack.
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1.What is erlotinib hydrochloride used for?
Answer : A drug used alone to treat certain types of non-small cell lung cancer and with gemcitabine hydrochloride to treat certain types of pancreatic cancer. It is also being studied in the treatment of other types of cancer.
2.Is erlotinib a chemotherapy drug?
Answer : Erlotinib is a non-chemotherapy drug for the treatment of advanced or metastatic NSCLC and is administered orally once a day. It successfully inhibits EGFR, a protein involved in the growth and development of cancers.
3.What is a known side effect of erlotinib?
Answer : Diarrhea, dry skin, muscle/joint pain, mouth sores, unusual eyelash growth, or eye dryness/redness/irritation may occur. Diarrhea can be severe. In some cases, your doctor may prescribe medication to relieve diarrhea. If any of these effects last or get worse, tell your doctor or pharmacist promptly.
4.Is erlotinib a protein?
Answer : Erlotinib, sold under the brand name Tarceva among others, is a medication used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer.
|Metabolism||Liver (mainly CYP3A4, less CYP1A2)|
|Elimination half-life||36.2 hrs (median)|
5. When is cisplatin used?
Answer : Cisplatin, a chemotherapy drug, is best known for curing testicular cancer. It is also used in the treatment of a wide range of other cancers, including lung, bladder, cervical, and ovarian cancers.
6.What is gefitinib used for?
Answer : Gefitinib is used to treat non-small cell lung cancer that has spread to other parts of the body in people with certain types of tumors. Gefitinib is in a class of medications called kinase inhibitors.
7. How long does erlotinib work?
Answer : Erlotinib is highly effective in the subset of patients carrying EGFR mutations. However, even these patients will eventually begin to show progression of their cancer after about 12 months of erlotinib therapy.
8. What class drug is erlotinib?
Answer : Erlotinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.
9. Does Tarceva shrink tumors?
Answer : Most patients respond to Tarceva, their tumors shrinking or even becoming undetectable. However, this effect is temporary. Most tumors come back, and most of them are ‘equipped’ with a new mutation in EGFR, known as T790M.
10. What are the side effects of cisplatin?
Answer : Side Effects
- Black, tarry stools.
- blood in urine or stools.
- burning, numbness, tingling, or painful sensations.
- change in frequency of urination or amount of urine.
- cough or hoarseness.
- difficulty in breathing.
- feeling of fullness in the ears.
- fever or chills.
11. How do you treat erlotinib rash?
Answer : The mainstay of treatment for the most common skin disorders associated with erlotinib–namely acneiform rash, xeroderma, pruritus, and paronychia–is topical steroids (at least strong class) together with emollients.
12. What is another name for erlotinib?
Answer : Erlotinib is a type of targeted cancer drug, and is also known by its brand name Tarceva (pronounced tar-see-vah). It is a treatment for: non small cell lung cancer (NSCLC) that has spread (advanced) advanced pancreatic cancer – alongside the chemotherapy drug gemcitabine.
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