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

Stem definition	Drug id	CAS RN
vinca alkaloids	2827	71486-22-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: vinorelbin ditartrate noranhydrovinblastine tartrate vinorelbine navelbin navelbine base 5'-anhydrovinblastine vinorelbine tartrate vinorelbine ditartrate navelbine vinorelbine base	A vinca alkaloid related to VINBLASTINE that is used as a first-line treatment for NON-SMALL CELL LUNG CANCER, or for advanced or metastatic BREAST CANCER refractory to treatment with ANTHRACYCLINES. Molecular weight: 778.95 Formula: C45H54N4O8 CLOGP: 5.94 LIPINSKI: 3 HAC: 12 HDO: 2 TPSA: 133.87 ALOGS: -4.81 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

vinorelbin ditartrate
noranhydrovinblastine tartrate
vinorelbine
navelbin
navelbine base
5'-anhydrovinblastine
vinorelbine tartrate
vinorelbine ditartrate
navelbine
vinorelbine base

A vinca alkaloid related to VINBLASTINE that is used as a first-line treatment for NON-SMALL CELL LUNG CANCER, or for advanced or metastatic BREAST CANCER refractory to treatment with ANTHRACYCLINES.

Molecular weight: 778.95
Formula: C45H54N4O8
CLOGP: 5.94
LIPINSKI: 3
HAC: 12
HDO: 2
TPSA: 133.87
ALOGS: -4.81
ROTB: 10

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	27 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	26 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	23 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	20 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	11 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1.00 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.87 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 23, 1994	FDA	PIERRE FABRE

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
Malignant neoplasm progression	795.21	21.92	397	15844	81724	63391057
Disease progression	723.70	21.92	427	15814	122331	63350450
Metastases to liver	444.61	21.92	182	16059	23457	63449324
Metastases to bone	412.98	21.92	167	16074	20852	63451929
Neutropenia	407.08	21.92	345	15896	174660	63298121
Palmar-plantar erythrodysaesthesia syndrome	306.91	21.92	139	16102	22876	63449905
Metastases to lung	270.09	21.92	107	16134	12643	63460138
Metastases to lymph nodes	243.58	21.92	88	16153	8070	63464711
Neoplasm progression	235.70	21.92	135	16106	36293	63436488
Mucosal inflammation	213.94	21.92	139	16102	46789	63425992

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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
Neutropenia	128.23	26.58	121	3918	156657	34796235
Disease progression	121.49	26.58	100	3939	107977	34844915
Febrile neutropenia	84.78	26.58	91	3948	136758	34816134
Malignant neoplasm progression	69.87	26.58	67	3972	87979	34864913
Off label use	59.11	26.58	141	3898	419383	34533509
Neutropenic sepsis	56.88	26.58	29	4010	13738	34939154
Febrile bone marrow aplasia	54.56	26.58	24	4015	8185	34944707
Pneumonitis	50.16	26.58	37	4002	33841	34919051
Neoplasm progression	40.34	26.58	28	4011	23272	34929620
Thrombocytopenia	39.21	26.58	67	3972	156180	34796712

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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
Malignant neoplasm progression	546.32	20.81	341	15876	135649	79592522
Disease progression	472.36	20.81	350	15867	184012	79544159
Neutropenia	366.50	20.81	366	15851	287344	79440827
Metastases to bone	254.83	20.81	116	16101	24311	79703860
Metastases to liver	229.49	20.81	113	16104	28201	79699970
Metastases to lung	227.25	20.81	98	16119	18065	79710106
Neoplasm progression	223.20	20.81	136	16081	51546	79676625
Palmar-plantar erythrodysaesthesia syndrome	171.36	20.81	98	16119	33036	79695135
Breast cancer metastatic	168.25	20.81	64	16153	8538	79719633
Mucosal inflammation	167.64	20.81	132	16085	75448	79652723

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01CA04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS Vinca alkaloids and analogues
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:47868	photosensitising agent
FDA CS	M0022674	Vinca Alkaloids
FDA EPC	N0000175612	Vinca Alkaloid
MeSH PA	D050256	Antimitotic Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D000972	Antineoplastic Agents, Phytogenic
MeSH PA	D050257	Tubulin Modulators

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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
Kaposi's sarcoma	off-label use	109385007
Neoplasm of endometrium	off-label use	123844007	DOID:1380
Small cell carcinoma of lung	off-label use	254632001	DOID:5409
Metastatic Breast Carcinoma	off-label use
Disorder of lung	contraindication	19829001	DOID:850
Infectious disease	contraindication	40733004
Gastrointestinal perforation	contraindication	51875005
Hepatic failure	contraindication	59927004
Interstitial pneumonia	contraindication	64667001

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.32	acidic
pKa2	13.35	acidic
pKa3	8.55	Basic
pKa4	7.39	Basic
pKa5	6.11	Basic

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Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Tubulin beta	Tumour-associated antigen	P07437 Q9H4B7 Q13885 Q9BVA1 Q13509 P04350 P68371 Q9BUF5 Q3ZCM7	TBB5_HUMAN TBB1_HUMAN TBB2A_HUMAN TBB2B_HUMAN TBB3_HUMAN TBB4A_HUMAN TBB4B_HUMAN TBB6_HUMAN TBB8_HUMAN	INHIBITOR			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6	DRUG MATRIX
Substance-K receptor	GPCR	P21452	NK2R_HUMAN		Ki	6.27	DRUG MATRIX

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External reference:

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ID	Source
GDF	PDB_CHEM_ID
004380	NDDF
004381	NDDF
108792008	SNOMEDCT_US
108794009	SNOMEDCT_US
114527	RXNORM
125317-39-7	SECONDARY_CAS_RN
2135	MMSL
372541004	SNOMEDCT_US
4020895	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Vinorelbine	HUMAN PRESCRIPTION DRUG LABEL	1	25021-204	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	27 sections
Vinorelbine	HUMAN PRESCRIPTION DRUG LABEL	1	45963-607	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	19 sections
Vinorelbine	HUMAN PRESCRIPTION DRUG LABEL	1	45963-607	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	19 sections
Vinorelbine	HUMAN PRESCRIPTION DRUG LABEL	1	45963-607	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	19 sections

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