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

Stem definition	Drug id	CAS RN
vinca alkaloids	2826	53643-48-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: eldisine desacetylvinblastine amide vindesine sulfate vindesine compound 112531	Vinblastine derivative with antineoplastic activity against CANCER. Major side effects are myelosuppression and neurotoxicity. Vindesine is used extensively in chemotherapy protocols (ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS). Molecular weight: 753.94 Formula: C43H55N5O7 CLOGP: 3.42 LIPINSKI: 2 HAC: 12 HDO: 5 TPSA: 164.82 ALOGS: -4.03 ROTB: 7

Molecule

Description

Molfile Inchi Smiles

Synonyms:

eldisine
desacetylvinblastine amide
vindesine sulfate
vindesine
compound 112531

Vinblastine derivative with antineoplastic activity against CANCER. Major side effects are myelosuppression and neurotoxicity. Vindesine is used extensively in chemotherapy protocols (ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS).

Molecular weight: 753.94
Formula: C43H55N5O7
CLOGP: 3.42
LIPINSKI: 2
HAC: 12
HDO: 5
TPSA: 164.82
ALOGS: -4.03
ROTB: 7

Drug dosage:

None

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.14 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	5 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	35 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1979	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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
Myelosuppression	484.06	60.35	106	1037	23597	63464282
Bone marrow failure	170.06	60.35	48	1095	29242	63458637
Leukopenia	83.04	60.35	36	1107	77254	63410625

FDA Adverse Event Reporting System (Male)

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
Myelosuppression	469.02	37.15	128	2146	19137	34935520
Bone marrow failure	276.39	37.15	94	2180	29159	34925498
Stomatitis	86.50	37.15	46	2228	42468	34912189
Leukopenia	64.98	37.15	44	2230	62812	34891845
Febrile neutropenia	62.04	37.15	59	2215	136790	34817867
Agranulocytosis	57.67	37.15	29	2245	23792	34930865
Large intestine infection	45.73	37.15	12	2262	1506	34953151
Pyrexia	43	37.15	77	2197	332936	34621721

FDA Adverse Event Reporting System (Geriatric)

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
Myelosuppression	891.46	39.94	229	3310	40067	79700782
Bone marrow failure	450.50	39.94	142	3397	50965	79689884
Leukopenia	142.34	39.94	79	3460	116434	79624415
Agranulocytosis	97.41	39.94	45	3494	44985	79695864
Febrile neutropenia	87.12	39.94	76	3463	230923	79509926
White blood cell count decreased	79.23	39.94	66	3473	188222	79552627
Pyrexia	74.36	39.94	118	3421	678591	79062258
Stomatitis	64.93	39.94	53	3486	146704	79594145
Granulocytopenia	50.39	39.94	19	3520	11412	79729437
Neutrophil count decreased	43.77	39.94	35	3504	93924	79646925
Large intestine infection	41.52	39.94	12	3527	3157	79737692
Acute myeloid leukaemia	40.50	39.94	22	3517	30863	79709986

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01CA03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS Vinca alkaloids and analogues
CHEBI has role	CHEBI:35610	antineoplastic agents
MeSH PA	D050256	Antimitotic Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D000972	Antineoplastic Agents, Phytogenic
MeSH PA	D050257	Tubulin Modulators

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

Disease	Relation	SNOMED_ID	DOID
Acute lymphoid leukemia	indication	91857003	DOID:9952
Chronic myeloid leukemia	indication	92818009	DOID:8552
Malignant tumor of lung	indication	363358000
Malignant melanoma	indication	372244006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.64	acidic
pKa2	13.81	acidic
pKa3	7.86	Basic
pKa4	6.98	Basic
pKa5	6.15	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		Km	4.61		WOMBAT-PK

External reference:

ID	Source
4025282	VUID
N0000171809	NUI
D01769	KEGG_DRUG
59917-39-4	SECONDARY_CAS_RN
4025282	VANDF
4025283	VANDF
C0042682	UMLSCUI
CHEBI:32295	CHEBI
CHEMBL238071	ChEMBL_ID
CHEMBL219146	ChEMBL_ID
CHEMBL3989543	ChEMBL_ID
CHEMBL2105882	ChEMBL_ID
D014751	MESH_DESCRIPTOR_UI
DB00309	DRUGBANK_ID
3927	INN_ID
RSA8KO39WH	UNII
40839	PUBCHEM_CID
11204	RXNORM
003505	NDDF
003506	NDDF
349851002	SNOMEDCT_US
395921004	SNOMEDCT_US
409198005	SNOMEDCT_US

Pharmaceutical products:

None