Lapatinib - Revision history

Prab at 08:46, 27 March 2025

2025-03-27T08:46:12Z

← Older revision		Revision as of 08:46, 27 March 2025
Line 6:		Line 6:
	[[File:Lapatinib (9738379442).png\|thumb\|'''Lapatinib''']]		[[File:Lapatinib (9738379442).png\|thumb\|'''Lapatinib''']]
	[[File:Lapatinib (9738130414).png\|thumb\|'''Lapatinib''']]		[[File:Lapatinib (9738130414).png\|thumb\|'''Lapatinib''']]


	<youtube>		<youtube>
Line 17:		Line 16:
	height=600		height=600
	</youtube>		</youtube>


	== '''What are the uses of this medicine?''' ==		== '''What are the uses of this medicine?''' ==
Line 30:		Line 28:
	* have gone through the change of life (postmenopausal), and		* have gone through the change of life (postmenopausal), and
	* who have [[metastatic]] breast cancer that is [[Hormone receptor-positive breast carcinoma\|hormone receptor-positive]], [[HER2\|HER2-positive]], and hormonal therapy is a treatment option for them.		* who have [[metastatic]] breast cancer that is [[Hormone receptor-positive breast carcinoma\|hormone receptor-positive]], [[HER2\|HER2-positive]], and hormonal therapy is a treatment option for them.


	== '''How does this medicine work?''' ==		== '''How does this medicine work?''' ==

	~~<youtube>~~
	~~title='''{{PAGENAME}}'''~~
	~~movie_url=http://www.youtube.com/v=jq5cqBeL73M~~
	~~embed_source_url=http://www.youtube.com/v=jq5cqBeL73M~~
	~~&rel=1~~
	~~wrap = yes~~
	~~width=750~~
	~~height=600~~
	~~</youtube>~~

	* Lapatinib (la pa' ti nib) is a '''selective inhibitor of two tyrosine kinase receptors which are associated with tumor growth and angiogenesis'''.		* Lapatinib (la pa' ti nib) is a '''selective inhibitor of two tyrosine kinase receptors which are associated with tumor growth and angiogenesis'''.
Line 49:		Line 36:
	* Lapatinib is one of several tyrosine kinase inhibitors that have been introduced into cancer [[chemotherapy]] and are specially directed at molecular abnormalities that occur in cancer cells.		* Lapatinib is one of several tyrosine kinase inhibitors that have been introduced into cancer [[chemotherapy]] and are specially directed at molecular abnormalities that occur in cancer cells.
	* '''Inhibition of these receptors can lead to dramatic reversal of progression the cancer''', although the efficacy is sometimes limited by the development of tumor resistance caused by mutations in the kinase.		* '''Inhibition of these receptors can lead to dramatic reversal of progression the cancer''', although the efficacy is sometimes limited by the development of tumor resistance caused by mutations in the kinase.


	== '''Who Should Not Use this medicine ?''' ==		== '''Who Should Not Use this medicine ?''' ==
Line 55:		Line 41:
	This mediicne cannot be used in patients:		This mediicne cannot be used in patients:
	* with known severe [[hypersensitivity]] (e.g., [[anaphylaxis]]) to this product or any of its components.		* with known severe [[hypersensitivity]] (e.g., [[anaphylaxis]]) to this product or any of its components.


	== '''What drug interactions can this medicine cause?''' ==		== '''What drug interactions can this medicine cause?''' ==
Line 63:		Line 48:
	* Avoid strong CYP3A4 inhibitors. If unavoidable, consider dose reduction of Tykerb in patients coadministered a strong CYP3A4 inhibitor.		* Avoid strong CYP3A4 inhibitors. If unavoidable, consider dose reduction of Tykerb in patients coadministered a strong CYP3A4 inhibitor.
	* Avoid strong CYP3A4 inducers. If unavoidable, consider gradual dose increase of Tykerb in patients coadministered a strong CYP3A4 inducer.		* Avoid strong CYP3A4 inducers. If unavoidable, consider gradual dose increase of Tykerb in patients coadministered a strong CYP3A4 inducer.


	== '''Is this medicine FDA approved?''' ==		== '''Is this medicine FDA approved?''' ==

	* Lapatinib received approval for use in the United States in 2007 for treatment of patients with advanced or [[metastatic]] breast cancer whose tumors over express [[HER2]] to be used in combination with [[capecitabine]]. Indications have been broadened somewhat since then.		* Lapatinib received approval for use in the United States in 2007 for treatment of patients with advanced or [[metastatic]] breast cancer whose tumors over express [[HER2]] to be used in combination with [[capecitabine]]. Indications have been broadened somewhat since then.


	== '''How should this medicine be used?''' ==		== '''How should this medicine be used?''' ==


	'''Recommended dosage:'''		'''Recommended dosage:'''
Line 92:		Line 74:
	* If you miss a dose of Tykerb, take your next dose at your regular time the next day.		* If you miss a dose of Tykerb, take your next dose at your regular time the next day.
	* If you take too much Tykerb, call your healthcare provider or go to the nearest hospital emergency room right away.		* If you take too much Tykerb, call your healthcare provider or go to the nearest hospital emergency room right away.


	== '''What are the dosage forms and brand names of this medicine?''' ==		== '''What are the dosage forms and brand names of this medicine?''' ==
Line 101:		Line 82:
	This medicine is available in fallowing brand namesː		This medicine is available in fallowing brand namesː
	* '''Tykerb'''		* '''Tykerb'''


	=='''What side effects can this medication cause?'''==		=='''What side effects can this medication cause?'''==
Line 133:		Line 113:
	* lung problems		* lung problems
	* severe skin reactions		* severe skin reactions


	==''' What special precautions should I follow?''' ==		==''' What special precautions should I follow?''' ==
Line 145:		Line 124:
	* Severe [[cutaneous]] reactions have been reported. Discontinue Tykerb if life-threatening reactions are suspected.		* Severe [[cutaneous]] reactions have been reported. Discontinue Tykerb if life-threatening reactions are suspected.
	* Based on its mechanism of action and findings in animal studies, Tykerb can cause fetal harm when administered to a pregnant woman. Advise patients of the potential risk to the fetus and to use effective contraception.		* Based on its mechanism of action and findings in animal studies, Tykerb can cause fetal harm when administered to a pregnant woman. Advise patients of the potential risk to the fetus and to use effective contraception.


	== '''What to do in case of emergency/overdose?''' ==		== '''What to do in case of emergency/overdose?''' ==
Line 157:		Line 135:
	* Because Tykerb is not significantly renally excreted and is highly bound to plasma proteins, [[hemodialysis]] would not be expected to be an effective method to enhance the elimination of lapatinib.		* Because Tykerb is not significantly renally excreted and is highly bound to plasma proteins, [[hemodialysis]] would not be expected to be an effective method to enhance the elimination of lapatinib.
	* Treatment of overdose with Tykerb should consist of general supportive measures.		* Treatment of overdose with Tykerb should consist of general supportive measures.


	== '''Can this medicine be used in pregnancy?''' ==		== '''Can this medicine be used in pregnancy?''' ==
Line 163:		Line 140:
	* Based on findings in animal studies and its mechanism of action, Tykerb can cause fetal harm when administered to a pregnant woman.		* Based on findings in animal studies and its mechanism of action, Tykerb can cause fetal harm when administered to a pregnant woman.
	* There are no available human data to inform of the drug-associated risks.		* There are no available human data to inform of the drug-associated risks.


	=='''Can this medicine be used in children?'''==		=='''Can this medicine be used in children?'''==

	* The safety and effectiveness of Tykerb in pediatric patients have not been established.		* The safety and effectiveness of Tykerb in pediatric patients have not been established.


	== '''What are the active and inactive ingredients in this medicine?''' ==		== '''What are the active and inactive ingredients in this medicine?''' ==
Line 174:		Line 149:
	* '''Active ingredient:''' Lapatinib.		* '''Active ingredient:''' Lapatinib.
	* '''Inactive ingredients:''' Tablet Core: Magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate. Coating: Orange film-coat: FD&C yellow No. 6/sunset yellow FCF aluminum lake, hypromellose, macrogol/PEG 400, polysorbate 80, titanium dioxide.		* '''Inactive ingredients:''' Tablet Core: Magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate. Coating: Orange film-coat: FD&C yellow No. 6/sunset yellow FCF aluminum lake, hypromellose, macrogol/PEG 400, polysorbate 80, titanium dioxide.


	== '''Who manufactures and distributes this medicine?''' ==		== '''Who manufactures and distributes this medicine?''' ==

	'''Distributed by:''' [[Novartis Pharmaceuticals]] Corporation, East Hanover, New Jersey		'''Distributed by:''' [[Novartis Pharmaceuticals]] Corporation, East Hanover, New Jersey


	== '''What should I know about storage and disposal of this medication?''' ==		== '''What should I know about storage and disposal of this medication?''' ==
Line 192:		Line 165:
	{{GlaxoSmithKline}}		{{GlaxoSmithKline}}
	{{Portal bar \| Medicine}}		{{Portal bar \| Medicine}}

	[[Category:Amines]]		[[Category:Amines]]
	[[Category:Anilines]]		[[Category:Anilines]]

Deepika vegiraju at 11:56, 20 August 2022

2022-08-20T11:56:02Z

New page

== '''What is Lapatinib?''' ==

* Lapatinib ('''Tykerb''') is a '''[[kinase inhibitor]]''' used in the therapy of advanced [[breast cancer]] and other [[solid tumors]].

[[File:Lapatinib.svg|thumb|'''Lapatinib''']]
[[File:Lapatinib (9738379442).png|thumb|'''Lapatinib''']]
[[File:Lapatinib (9738130414).png|thumb|'''Lapatinib''']]

<youtube>
title='''{{PAGENAME}}'''
movie_url=http://www.youtube.com/v/v=KdEU3txPAx4
embed_source_url=http://www.youtube.com/v/v=KdEU3txPAx4
&rel=1
wrap = yes
width=750
height=600
</youtube>

== '''What are the uses of this medicine?''' ==

Lapatinib ('''Tykerb''') medicine used:
* with the medicine [[capecitabine]] to treat people with [[breast cancer]] that is advanced or that has spread to other parts of the body ([[metastatic]]), and:
* that is HER2-positive (tumors that produce large amounts of a protein called [[Human epidermal growth factor receptor 2|human epidermal growth factor receptor-2]]), and
* who have already had certain other breast cancer treatments
* Before taking Tykerb with [[capecitabine]], your breast cancer should have gotten worse (progressed) with the medicine [[trastuzumab]].

with the medicine [[letrozole]] to treat women who:
* have gone through the change of life (postmenopausal), and
* who have [[metastatic]] breast cancer that is [[Hormone receptor-positive breast carcinoma|hormone receptor-positive]], [[HER2|HER2-positive]], and hormonal therapy is a treatment option for them.

== '''How does this medicine work?''' ==

<youtube>
title='''{{PAGENAME}}'''
movie_url=http://www.youtube.com/v=jq5cqBeL73M
embed_source_url=http://www.youtube.com/v=jq5cqBeL73M
&rel=1
wrap = yes
width=750
height=600
</youtube>

* Lapatinib (la pa' ti nib) is a '''selective inhibitor of two tyrosine kinase receptors which are associated with tumor growth and angiogenesis'''.
* Lapatinib has '''special activity against the epidermal growth factor receptor (EGFR) and the human epidermal group factor receptor-2 (HER2)'''.
* Tyrosine kinase receptors are often mutated and over expressed in cancer cells, causing unregulated cell growth and [[proliferation]].
* Lapatinib is one of several tyrosine kinase inhibitors that have been introduced into cancer [[chemotherapy]] and are specially directed at molecular abnormalities that occur in cancer cells.
* '''Inhibition of these receptors can lead to dramatic reversal of progression the cancer''', although the efficacy is sometimes limited by the development of tumor resistance caused by mutations in the kinase.

== '''Who Should Not Use this medicine ?''' ==

This mediicne cannot be used in patients:
* with known severe [[hypersensitivity]] (e.g., [[anaphylaxis]]) to this product or any of its components.

== '''What drug interactions can this medicine cause?''' ==

* If Tykerb is administered with drugs that inhibit P-gp, increased concentrations of lapatinib are likely, and caution should be exercised.
* Tykerb is likely to increase exposure to concomitantly administered drugs which are substrates of CYP3A4, CYP2C8, or P-glycoprotein (ABCB1).
* Avoid strong CYP3A4 inhibitors. If unavoidable, consider dose reduction of Tykerb in patients coadministered a strong CYP3A4 inhibitor.
* Avoid strong CYP3A4 inducers. If unavoidable, consider gradual dose increase of Tykerb in patients coadministered a strong CYP3A4 inducer.

== '''Is this medicine FDA approved?''' ==

* Lapatinib received approval for use in the United States in 2007 for treatment of patients with advanced or [[metastatic]] breast cancer whose tumors over express [[HER2]] to be used in combination with [[capecitabine]]. Indications have been broadened somewhat since then.

== '''How should this medicine be used?''' ==

'''Recommended dosage:'''
'''HER2-Positive Metastatic Breast Cancer:'''
* The recommended dosage of Tykerb for advanced or metastatic breast cancer is 1,250 mg (5 tablets) given orally once daily on Days 1-21 continuously in combination with capecitabine 2,000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21-day cycle.

'''Hormone Receptor-Positive, HER2-Positive Metastatic Breast Cancer:'''
* The recommended dose of Tykerb for hormone receptor-positive, HER2-positive metastatic breast cancer is 1,500 mg (6 tablets) given orally once daily continuously in combination with [[letrozole]].
* When Tykerb is coadministered with letrozole, the recommended dose of letrozole is 2.5 mg once daily.

* Modify dose for cardiac and other toxicities, severe hepatic impairment, [[diarrhea]], and CYP3A4 drug interactions.

'''Administration:'''
* For people with advanced or metastatic breast cancer, Tykerb and [[capecitabine]] are taken in 21-day cycles. The usual dose of Tykerb is 1,250 mg (5 tablets) taken by mouth all at the same time, 1 time a day on days 1 to 21.
* Your healthcare provider will tell you the dose of capecitabine you should take and when you should take it.
* Take capecitabine with food or within 30 minutes after food.
* For people with hormone receptor-positive, HER2-positive breast cancer, Tykerb and [[letrozole]] are taken every day. The usual dose of Tykerb is 1,500 mg (6 tablets) taken by mouth all at the same time, 1 time a day. Your healthcare provider will tell you the dose of letrozole you should take and when you should take it.
* Take Tykerb at least 1 hour before, or at least 1 hour after a meal.
* Avoid eating or drinking [[grapefruit]] products during treatment with Tykerb.
* If you miss a dose of Tykerb, take your next dose at your regular time the next day.
* If you take too much Tykerb, call your healthcare provider or go to the nearest hospital emergency room right away.

== '''What are the dosage forms and brand names of this medicine?''' ==

This medicine is available in fallowing doasage form:
* As 250 mg tablets

This medicine is available in fallowing brand namesː
* '''Tykerb'''

=='''What side effects can this medication cause?'''==

The most common side effects of this medicine include:
'''Common side effects of Tykerb in combination with [[capecitabine]] or [[letrozole]] include:'''
* [[diarrhea]]
* red, painful hands and feet
* [[nausea]]
* rash
* vomiting
* inflamed mouth, digestive tract and airways
* [[mouth sores]]
* headache
* unusual hair loss or thinning
* shortness of breath
* dry skin
* itching
* tiredness
* painful arms, legs and back
* loss of appetite
* indigestion
* [[nose bleeds]]
* nail disorders such as nail bed changes, nail pain, infection and swelling of the cuticles
* difficulty sleeping

Tykerb may cause serious side effects, including:
* heart problems
* liver problems
* [[diarrhea]]
* lung problems
* severe skin reactions

==''' What special precautions should I follow?''' ==

* Decreases in [[left ventricular ejection fraction]] (LVEF) have been reported. Confirm normal LVEF before starting Tykerb and continue evaluations during treatment.
* Tykerb has been associated with [[hepatotoxicity]]. Monitor liver function tests before initiation of treatment, every 4 to 6 weeks during treatment, and as clinically indicated. Discontinue and do not restart Tykerb if patients experience severe changes in liver function tests.
* Hepatotoxicity [[[alanine aminotransferase]] (ALT) or [[aspartate aminotransferase]] (AST) greater than 3 times the upper limit of normal (ULN) and total bilirubin greater than 2 times the ULN] has been observed. Dose reduction in patients with severe hepatic impairment should be considered.
* [[Diarrhea]], including severe diarrhea, has been reported during treatment. Manage with antidiarrheal agents, and replace fluids and electrolytes if severe.
* Tykerb has been associated with [[interstitial lung disease]] and [[pneumonitis]]. Discontinue Tykerb if patients experience severe pulmonary symptoms.
* Tykerb may prolong the QT interval in some patients. Consider electrocardiogram (ECG) and electrolyte monitoring.
* Severe [[cutaneous]] reactions have been reported. Discontinue Tykerb if life-threatening reactions are suspected.
* Based on its mechanism of action and findings in animal studies, Tykerb can cause fetal harm when administered to a pregnant woman. Advise patients of the potential risk to the fetus and to use effective contraception.

== '''What to do in case of emergency/overdose?''' ==

'''Symptoms of overdosage may include:'''
* Asymptomatic and symptomatic cases of overdose have been reported.
* Symptoms observed include Tykerb-associated events and in some cases sore scalp, sinus tachycardia (with otherwise normal ECG), and/or mucosal inflammation.

'''Treatment of overdosage:'''
* There is no known antidote for overdoses of Tykerb.
* Because Tykerb is not significantly renally excreted and is highly bound to plasma proteins, [[hemodialysis]] would not be expected to be an effective method to enhance the elimination of lapatinib.
* Treatment of overdose with Tykerb should consist of general supportive measures.

== '''Can this medicine be used in pregnancy?''' ==

* Based on findings in animal studies and its mechanism of action, Tykerb can cause fetal harm when administered to a pregnant woman.
* There are no available human data to inform of the drug-associated risks.

=='''Can this medicine be used in children?'''==

* The safety and effectiveness of Tykerb in pediatric patients have not been established.

== '''What are the active and inactive ingredients in this medicine?''' ==

* '''Active ingredient:''' Lapatinib.
* '''Inactive ingredients:''' Tablet Core: Magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate. Coating: Orange film-coat: FD&C yellow No. 6/sunset yellow FCF aluminum lake, hypromellose, macrogol/PEG 400, polysorbate 80, titanium dioxide.

== '''Who manufactures and distributes this medicine?''' ==

'''Distributed by:''' [[Novartis Pharmaceuticals]] Corporation, East Hanover, New Jersey

== '''What should I know about storage and disposal of this medication?''' ==

* Store Tykerb at room temperature between 68°F to 77°F (20°C to 25°C).
* Do not keep medicine that is out of date or that you no longer need.

{{cancer drugs}}
{{coststubd}}
{{Extracellular chemotherapeutic agents}}
{{Growth factor receptor modulators}}
{{GlaxoSmithKline}}
{{Portal bar | Medicine}}

[[Category:Amines]]
[[Category:Anilines]]
[[Category:Aromatic amines]]
[[Category:Chloroarenes]]
[[Category:Furans]]
[[Category:Fluoroarenes]]
[[Category:Phenol ethers]]
[[Category:Quinazolines]]
[[Category:Receptor tyrosine kinase inhibitors]]
[[Category:Sulfones]]
[[Category:GlaxoSmithKline brands]]
[[Category:Novartis brands]]