Tarceva

(Erlotinib Hydrochloride)

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Tarceva Prescribing Information

Indications and Usage, Non-Small Cell Lung Cancer (NSCLC) (

1.1 Non-Small Cell Lung Cancer (NSCLC)

TARCEVA^®is indicated for:

• The treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen

[see Clinical Studies].

Limitations of use:

• Safety and efficacy of TARCEVA have not been established in patients with NSCLC whose tumors have other EGFR mutations

[see Clinical Studies].

• TARCEVA is not recommended for use in combination with platinum-based chemotherapy

[see Clinical Studies]

) 10/2016

Dosage and Administration (

2.1 Selection of Patients with Metastatic NSCLC

Select patients for the treatment of metastatic NSCLC with TARCEVA based on the presence of EGFR exon 19 deletions or exon 21 (L858R) substitution mutations in tumor or plasma specimens

[See Clinical Studies]

. If these mutations are not detected in a plasma specimen, test tumor tissue if available. Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics.

) 06/2016

Dosage and Administration, Dose Modifications (

2.4 Dose Modifications

Adverse Reactions
PulmonaryFor additional information see Warnings and Precautions .	Interstitial Lung Disease (ILD)	Discontinue TARCEVA
	During diagnostic evaluation for possible ILD	Withhold TARCEVAReduce TARCEVA by 50 mg decrements when restarting therapy following withholding treatment for a dose-limiting toxicity that has resolved to baseline or grade ≤ 1.
Hepatic	Severe hepatic toxicity that does not improve significantly or resolve within three weeks	Discontinue TARCEVA
	In patients with pre-existing hepatic impairment or biliary obstruction for doubling of bilirubin or tripling of transaminases values over baseline	Withhold TARCEVA and consider discontinuation
	In patients without pre-existing hepatic impairment for total bilirubin levels greater than 3 times the upper limit of normal or transaminases greater than 5 times the upper limit of normal	Withhold TARCEVA and consider discontinuation
Renal	For severe (CTCAE grade 3 to 4) renal toxicity	Withhold TARCEVA and consider discontinuation
Gastrointestinal	Gastrointestinal perforation	Discontinue TARCEVA
Gastrointestinal	For persistent severe diarrhea not responsive to medical management (e.g., loperamide)	Withhold TARCEVA
Skin	Severe bullous, blistering or exfoliating skin conditions	Discontinue TARCEVA
Skin	For severe rash not responsive to medical management	Withhold TARCEVA
Ocular	Corneal perforation or severe ulceration	Discontinue TARCEVA
	For keratitis of (NCI-CTC version 4.0) grade 3-4 or for grade 2 lasting more than 2 weeks	Withhold TARCEVA
	For acute/worsening ocular disorders such as eye pain	Withhold TARCEVA and consider discontinuation
Drug Interactions
CYP3A4 inhibitorsFor additional information see Drug Interactions .	If severe reactions occur with concomitant use of strong CYP3A4 inhibitors [such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin (TAO), voriconazole, or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., ciprofloxacin)	Reduce TARCEVA by 50 mg decrements; avoid concomitant use if possible
CYP3A4 inducers	Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John’s Wort	Increase TARCEVA by 50 mg increments at 2-week intervals to a maximum of 450 mg as tolerated. Avoid concomitant use if possible
Concurrent Cigarette Smoking For additional information see Clinical Pharmacology .	Concurrent cigarette smoking	Increase TARCEVA by 50 mg increments at 2-week intervals to a maximum of 300 mg. Immediately reduce the dose of TARCEVA to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking
Proton Pump inhibitors	Separation of doses may not eliminate the interaction since proton pump inhibitors affect the pH of the upper GI tract for an extended period	Avoid concomitant use if possible
H₂-receptor antagonists	If treatment with an H₂-receptor antagonist such as ranitidine is required, separate dosing.	TARCEVA 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
Antacids	The effect of antacids on erlotinib pharmacokinetics has not been evaluated.	The antacid dose and the TARCEVA dose should be separated by several hours, if an antacid is necessary

) 05/2016

Warnings and Precautions, Cerebrovascular Accident (

5.6 Cerebrovascular Accident

In the pancreatic carcinoma trial, seven patients in the TARCEVA/gemcitabine group developed cerebrovascular accidents (incidence: 2.5%). One of these was hemorrhagic and was the only fatal event. In comparison, in the placebo/gemcitabine group there were no cerebrovascular accidents. The pooled incidence of cerebrovascular accident in the 3 monotherapy lung cancer studies was 0.6% in the TARCEVA arms and not higher than that observed in the control arms.

) 10/2016

Warnings and Precautions, Embryo-fetal Toxicity (

5.10 Embryo-fetal Toxicity

Based on animal data and its mechanism of action, TARCEVA can cause fetal harm when administered to a pregnant woman. When given during organogenesis, erlotinib administration resulted in embryo-fetal lethality and abortion in rabbits at exposures approximately 3 times the exposure at the recommended human daily dose of 150 mg. Advise pregnant women of the potential risk to a fetus.

Advise females of reproductive potential to use effective contraception during therapy and for one month after the last dose of TARCEVA

[see Use in Specific Populations and (

8.3

), Clinical Pharmacology]

) 10/2016

TARCEVA is a kinase inhibitor indicated for:

•The treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen. (
1.1 Non-Small Cell Lung Cancer (NSCLC)
TARCEVA^®is indicated for:
•    The treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen
[see Clinical Studies].
Limitations of use:
•    Safety and efficacy of TARCEVA have not been established in patients with NSCLC whose tumors have other EGFR mutations
[see Clinical Studies].

•    TARCEVA is not recommended for use in combination with platinum-based chemotherapy
[see Clinical Studies]
.
)
•First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine. (
1.2 Pancreatic Cancer
TARCEVA in combination with gemcitabine is indicated for the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer
[see Clinical Studies]
.
)

Limitations of Use:

•Safety and efficacy of TARCEVA have not been established in patients with NSCLC whose tumors have other EGFR mutations. (
1.1 Non-Small Cell Lung Cancer (NSCLC)
TARCEVA^®is indicated for:
•    The treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen
[see Clinical Studies].
Limitations of use:
•    Safety and efficacy of TARCEVA have not been established in patients with NSCLC whose tumors have other EGFR mutations
[see Clinical Studies].

•    TARCEVA is not recommended for use in combination with platinum-based chemotherapy
[see Clinical Studies]
.
)
•TARCEVA is not recommended for use in combination with platinum-based chemotherapy. (
1.1 Non-Small Cell Lung Cancer (NSCLC)
TARCEVA^®is indicated for:
•    The treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen
[see Clinical Studies].
Limitations of use:
•    Safety and efficacy of TARCEVA have not been established in patients with NSCLC whose tumors have other EGFR mutations
[see Clinical Studies].

•    TARCEVA is not recommended for use in combination with platinum-based chemotherapy
[see Clinical Studies]
.
)

•NSCLC: 150 mg orally, on an empty stomach, once daily. (
2.2 Recommended Dose – NSCLC
The recommended daily dose of TARCEVA for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
)
•Pancreatic cancer: 100 mg orally, on an empty stomach, once daily. (
2.3 Recommended Dose – Pancreatic Cancer
The recommended daily dose of TARCEVA for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take TARCEVA on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs
[see Clinical Studies]
.
)

25 mg tablets: round, biconvex face and straight sides, white film-coated, printed in orange with “T” and “25” on one side and plain on other side.

100 mg tablets: round, biconvex face and straight sides, white film-coated, printed in gray with “T” and “100” on one side and plain on other side.

150 mg tablets: round, biconvex face and straight sides, white film-coated, printed in maroon with “T” and “150” on one side and plain on other side.

Lactation: Do not breastfeed (

8.2 Lactation

Risk Summary

There are no data on the presence of erlotinib in human milk, or the effects of erlotinib on the breastfed infant or on milk production. Because of the potential for serious adverse reactions in breastfed infants from TARCEVA, including interstitial lung disease, hepatotoxicity, bullous and exfoliative skin disorders, microangiopathic hemolytic anemia with thrombocytopenia, ocular disorders, and diarrhea. Advise a lactating woman not to breastfeed during treatment with TARCEVA and for 2 weeks after the final dose.

)

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