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erlotinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	1045	183321-74-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: erlotinib hydrochloride tarceva erlotinib CP-358,774-01 OSI-774 erlotinib HCl	A quinazoline derivative and ANTINEOPLASTIC AGENT that functions as a PROTEIN KINASE INHIBITOR for EGFR associated tyrosine kinase. It is used in the treatment of NON-SMALL CELL LUNG CANCER. Molecular weight: 393.44 Formula: C22H23N3O4 CLOGP: 4.19 LIPINSKI: 0 HAC: 7 HDO: 1 TPSA: 74.73 ALOGS: -4.64 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

erlotinib hydrochloride
tarceva
erlotinib
CP-358,774-01
OSI-774
erlotinib HCl

A quinazoline derivative and ANTINEOPLASTIC AGENT that functions as a PROTEIN KINASE INHIBITOR for EGFR associated tyrosine kinase. It is used in the treatment of NON-SMALL CELL LUNG CANCER.

Molecular weight: 393.44
Formula: C22H23N3O4
CLOGP: 4.19
LIPINSKI: 0
HAC: 7
HDO: 1
TPSA: 74.73
ALOGS: -4.64
ROTB: 10

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.15	g	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	6.50 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	59 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	5.45 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	1.69 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.77 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.30 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.07 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Nov. 18, 2004	FDA	OSI PHARMS
Sept. 19, 2005	EMA	ROCHE REGISTRATION GMBH

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	5963.47	20.84	2794	20140	371587	63094501
Disease progression	982.69	20.84	588	22346	122170	63343918
Rash	679.95	20.84	916	22018	559955	62906133
Diarrhoea	576	20.84	965	21969	714401	62751687
Malignant neoplasm progression	533.34	20.84	345	22589	81776	63384312
Dermatitis acneiform	381.56	20.84	119	22815	4877	63461211
Drug resistance	313.65	20.84	157	22777	22776	63443312
Metastases to central nervous system	222.27	20.84	104	22830	13001	63453087
Dry skin	203.91	20.84	167	22767	56720	63409368
Paronychia	170.03	20.84	67	22867	5498	63460590

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	5821.52	17.39	3320	18137	394729	34540745
Rash	914.03	17.39	883	20574	221869	34713605
Disease progression	752.34	17.39	581	20876	107496	34827978
Dermatitis acneiform	281.26	17.39	115	21342	6074	34929400
Malignant neoplasm progression	280.07	17.39	306	21151	87740	34847734
Diarrhoea	218.77	17.39	626	20831	389286	34546188
Neoplasm malignant	204.30	17.39	136	21321	19769	34915705
Dehydration	117.17	17.39	251	21206	129718	34805756
Metastases to central nervous system	111.52	17.39	67	21390	8138	34927336
Drug resistance	103.58	17.39	102	21355	25825	34909649

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Rash	802.18	16.46	961	25107	577397	79140923
Malignant neoplasm progression	770.75	16.46	505	25563	135485	79582835
Disease progression	630.47	16.46	504	25564	183858	79534462
Diarrhoea	535.53	16.46	994	25074	879495	78838825
Dermatitis acneiform	533.50	16.46	177	25891	9816	79708504
Drug resistance	480.39	16.46	247	25821	41966	79676354
Death	376.10	16.46	666	25402	565848	79152472
Metastases to central nervous system	231.11	16.46	111	25957	16264	79702056
EGFR gene mutation	200.02	16.46	43	26025	421	79717899
Dehydration	185.01	16.46	308	25760	247879	79470441

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EB02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:37699	protein kinase inhibitors
CHEBI has role	CHEBI:74440	EGFR antagonoists
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175076	Protein Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Non-small cell lung cancer	indication	254637007	DOID:3908
Adenocarcinoma of pancreas	indication	700423003	DOID:4074
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Myocardial infarction	contraindication	22298006	DOID:5844
Dehydration	contraindication	34095006
Hypokalemia	contraindication	43339004
Hepatorenal syndrome	contraindication	51292008	DOID:11823
Fibrosis of lung	contraindication	51615001	DOID:3770
Gastrointestinal perforation	contraindication	51875005
Hemolytic anemia	contraindication	61261009	DOID:583

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.01	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	INHIBITOR	IC50	9.22	WOMBAT-PK	CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	6.22	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	6.15	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	6.89	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	5.85	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	7.24	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	5.89	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	5.74	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	6.15	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	6.60	CHEMBL

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External reference:

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ID	Source
AQ4	PDB_CHEM_ID
008759	NDDF
008760	NDDF
176870	PUBCHEM_CID
183319-69-9	SECONDARY_CAS_RN
19073	MMSL
248186	MMSL
337525	RXNORM
4021511	VANDF
414122006	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7662	TABLET, FILM COATED	25 mg	ORAL	ANDA	24 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7663	TABLET, FILM COATED	100 mg	ORAL	ANDA	24 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7664	TABLET, FILM COATED	150 mg	ORAL	ANDA	24 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	51991-890	TABLET, FILM COATED	25 mg	ORAL	ANDA	28 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	51991-890	TABLET, FILM COATED	25 mg	ORAL	ANDA	28 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	51991-891	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	51991-891	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	51991-892	TABLET, FILM COATED	150 mg	ORAL	ANDA	28 sections
Erlotinib	HUMAN PRESCRIPTION DRUG LABEL	1	51991-892	TABLET, FILM COATED	150 mg	ORAL	ANDA	28 sections
Erlotinib	Human Prescription Drug Label	1	59651-530	TABLET, FILM COATED	25 mg	ORAL	ANDA	25 sections

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