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

Stem definition	Drug id	CAS RN
proteasome inhibitors	391	179324-69-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: LDP-341 PS-341 bortezomib velcade radiciol	A pyrazine and boronic acid derivative that functions as a reversible PROTEASOME INHIBITOR. It is used as an ANTINEOPLASTIC AGENT in the treatment of MULTIPLE MYELOMA and MANTLE CELL LYMPHOMA. Molecular weight: 384.24 Formula: C19H25BN4O4 CLOGP: 0.80 LIPINSKI: 0 HAC: 8 HDO: 4 TPSA: 124.44 ALOGS: -3.86 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

LDP-341
PS-341
bortezomib
velcade
radiciol

A pyrazine and boronic acid derivative that functions as a reversible PROTEASOME INHIBITOR. It is used as an ANTINEOPLASTIC AGENT in the treatment of MULTIPLE MYELOMA and MANTLE CELL LYMPHOMA.

Molecular weight: 384.24
Formula: C19H25BN4O4
CLOGP: 0.80
LIPINSKI: 0
HAC: 8
HDO: 4
TPSA: 124.44
ALOGS: -3.86
ROTB: 9

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
S (Water solubility)	3.30 mg/mL	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	19 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	18 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	10 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.17 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.08 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

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Date	Agency	Company
Aug. 22, 2019	PMDA	Janssen Pharmaceutical K.K.
May 13, 2003	FDA	MILLENNIUM PHARMS
Nov. 14, 2019	EMA	FRESENIUS KABI DEUTSCHLAND GMBH

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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
Neuropathy peripheral	2595.04	14.08	1565	65225	112102	63310130
Plasma cell myeloma	1523.98	14.08	747	66043	35158	63387074
Plasma cell myeloma recurrent	719.15	14.08	224	66566	2989	63419243
Thrombocytopenia	693.96	14.08	824	65966	150333	63271899
Disease progression	494.69	14.08	627	66163	122131	63300101
Platelet count decreased	450.33	14.08	582	66208	115540	63306692
Diarrhoea	414.45	14.08	1663	65127	713703	62708529
Plasmacytoma	345.14	14.08	122	66668	2457	63419775
Neutropenia	325.70	14.08	626	66164	174379	63247853
Polyneuropathy	323.95	14.08	198	66592	14391	63407841

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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
Neuropathy peripheral	2654.45	12.95	1873	76342	81390	34797326
Plasma cell myeloma	1487.00	12.95	1010	77205	41027	34837689
Plasma cell myeloma recurrent	793.02	12.95	318	77897	4147	34874569
Polyneuropathy	566.76	12.95	375	77840	14521	34864195
Thrombocytopenia	493.48	12.95	1082	77133	155165	34723551
Platelet count decreased	407.42	12.95	855	77360	118862	34759854
Disease progression	378.32	12.95	781	77434	107296	34771420
Pneumonia	327.80	12.95	1637	76578	360990	34517726
Plasmacytoma	313.77	12.95	157	78058	3534	34875182
Plasma cell myeloma refractory	308.73	12.95	95	78120	520	34878196

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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
Neuropathy peripheral	3691.30	12.17	2395	114705	138910	79488378
Plasma cell myeloma	2292.95	12.17	1248	115852	52011	79575277
Plasma cell myeloma recurrent	1501.27	12.17	472	116628	4529	79622759
Thrombocytopenia	1210.73	12.17	1706	115394	263553	79363735
Disease progression	855.22	12.17	1196	115904	183166	79444122
Polyneuropathy	840.93	12.17	493	116607	23658	79603630
Platelet count decreased	795.14	12.17	1189	115911	193475	79433813
Pneumonia	683.40	12.17	2322	114778	657924	78969364
Plasmacytoma	612.47	12.17	234	116866	4169	79623119
Plasma cell myeloma refractory	457.14	12.17	120	116980	552	79626736

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XG01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Proteasome inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:35820	antiprotozoal drugs
CHEBI has role	CHEBI:37670	protease inhibitors
CHEBI has role	CHEBI:52726	proteasome inhibitors
FDA EPC	N0000175604	Proteasome Inhibitor
FDA MoA	N0000175075	Proteasome Inhibitors
MeSH PA	D000970	Antineoplastic Agents

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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
Systemic AL amyloidosis	indication	23132008
Multiple myeloma	indication	109989006	DOID:9538
Mantle cell lymphoma	indication	443487006
Orthostatic hypotension	contraindication	28651003
Dehydration	contraindication	34095006
Low blood pressure	contraindication	45007003
Chronic heart failure	contraindication	48447003
Disorder of cardiovascular system	contraindication	49601007	DOID:1287
Interstitial pneumonia	contraindication	64667001
Adult respiratory distress syndrome	contraindication	67782005	DOID:11394

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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	9.39	acidic
pKa2	12.09	acidic
pKa3	13.65	acidic
pKa4	2.9	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
3.5MG/1.4ML (2.5MG/ML)	BORTEZOMIB	MAIA PHARMS INC	N215331	July 27, 2022	RX	SOLUTION	INTRAVENOUS	11679119	Sept. 23, 2042	TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA
3.5MG/1.4ML (2.5MG/ML)	BORTEZOMIB	MAIA PHARMS INC	N215331	July 27, 2022	RX	SOLUTION	INTRAVENOUS	11679119	Sept. 23, 2042	TREATMENT OF ADULT PATIENTS WITH MULTIPLE MYELOMA
3.5MG/3.5ML (1MG/ML)	BORTEZOMIB	MAIA PHARMS INC	N215331	July 27, 2022	DISCN	SOLUTION	INTRAVENOUS	11679119	Sept. 23, 2042	TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA
3.5MG/3.5ML (1MG/ML)	BORTEZOMIB	MAIA PHARMS INC	N215331	July 27, 2022	DISCN	SOLUTION	INTRAVENOUS	11679119	Sept. 23, 2042	TREATMENT OF ADULT PATIENTS WITH MULTIPLE MYELOMA

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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
Proteasome subunit alpha type-1	Enzyme	P25786	PSA1_HUMAN	INHIBITOR	Ki	9.21	WOMBAT-PK	CHEMBL
Proteasome subunit beta type-1	Enzyme	P20618	PSB1_HUMAN	INHIBITOR	IC50	7.28	CHEMBL	CHEMBL
Proteasome subunit beta type-2	Enzyme	P49721	PSB2_HUMAN	INHIBITOR	IC50	6.23	CHEMBL	CHEMBL
Proteasome subunit beta type-5	Enzyme	P28074	PSB5_HUMAN	INHIBITOR	Ki	9.26	CHEMBL	CHEMBL
Proteasome subunit beta type-8	Enzyme	P28062	PSB8_HUMAN	INHIBITOR	IC50	8.09	CHEMBL	CHEMBL
Prothrombin	Enzyme	P00734	THRB_HUMAN		Ki	4.89	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	5.16	CHEMBL
Carbonic anhydrase 5B, mitochondrial	Enzyme	Q9Y2D0	CAH5B_HUMAN		Ki	5.17	CHEMBL
Carbonic anhydrase 7	Enzyme	P43166	CAH7_HUMAN		Ki	5.16	CHEMBL
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		Ki	4.75	WOMBAT-PK

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External reference:

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ID	Source
BO2	PDB_CHEM_ID
009985	NDDF
17263	MMSL
233935	MMSL
356733	RXNORM
387447	PUBCHEM_CID
398907002	SNOMEDCT_US
4021393	VUID
4021393	VANDF
407097007	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
bortezomib	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9098	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	3.50 mg	INTRAVENOUS	ANDA	31 sections
Bortezomib	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1700	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	3.50 mg	INTRAVENOUS	ANDA	33 sections
BORTEZOMIB	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1703	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	2.50 mg	INTRAVENOUS	NDA	34 sections
BORTEZOMIB	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1703	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	2.50 mg	INTRAVENOUS	NDA	34 sections
BORTEZOMIB	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1704	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	NDA	34 sections
BORTEZOMIB	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1704	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	1 mg	INTRAVENOUS	NDA	34 sections
bortezomib	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3258	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	3.50 mg	INTRAVENOUS	ANDA	27 sections
BORTEZOMIB	HUMAN PRESCRIPTION DRUG LABEL	1	10019-991	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	3.50 mg	INTRAVENOUS	ANDA	28 sections
BORTEZOMIB	HUMAN PRESCRIPTION DRUG LABEL	1	10019-991	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	3.50 mg	INTRAVENOUS	ANDA	28 sections
BORTEZOMIB	HUMAN PRESCRIPTION DRUG LABEL	1	25021-244	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	3.50 mg	INTRAVENOUS	ANDA	31 sections

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