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

Stem definition	Drug id	CAS RN
proteasome inhibitors	5067	1072833-77-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ixazomib ixazomib citrate MLN2238 MLN9708 ninlaro	an oral proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708 Molecular weight: 361.03 Formula: C14H19BCl2N2O4 CLOGP: 1.10 LIPINSKI: 0 HAC: 6 HDO: 4 TPSA: 98.66 ALOGS: -4.47 ROTB: 7 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ixazomib
ixazomib citrate
MLN2238
MLN9708
ninlaro

an oral proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708

Molecular weight: 361.03
Formula: C14H19BCl2N2O4
CLOGP: 1.10
LIPINSKI: 0
HAC: 6
HDO: 4
TPSA: 98.66
ALOGS: -4.47
ROTB: 7

Status: ONP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	97 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	3.61 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	0.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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Date	Agency	Company
March 30, 2017	PMDA	Takeda Pharmaceutical Company Limited
Nov. 20, 2015	FDA	MILLENNIUM PHARMS
Nov. 21, 2016	EMA	Takeda Pharma A/S

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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
Diarrhoea	888.10	20.69	1196	22376	714170	62751280
Neuropathy peripheral	622.95	20.69	434	23138	113233	63352217
Death	556.19	20.69	687	22885	373694	63091756
Thrombocytopenia	335.78	20.69	343	23229	150814	63314636
Platelet count decreased	291.95	20.69	282	23290	115840	63349610
Pneumonia	252.12	20.69	535	23037	456232	63009218
Adverse event	243.05	20.69	201	23371	67358	63398092
Off label use	234.65	20.69	661	22911	673801	62791649
Plasma cell myeloma recurrent	220.42	20.69	71	23501	3142	63462308
Product physical issue	200.98	20.69	74	23498	4906	63460544

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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	519.40	20.13	905	21045	397144	34537837
Neuropathy peripheral	514.71	20.13	422	21528	82841	34852140
Pneumonia	321.30	20.13	702	21248	361925	34573056
Diarrhoea	305.62	20.13	719	21231	389193	34545788
Adverse event	281.89	20.13	165	21785	18712	34916269
Off label use	271.19	20.13	719	21231	418805	34516176
Platelet count decreased	223.01	20.13	322	21628	119395	34815586
Plasma cell myeloma recurrent	221.71	20.13	89	21861	4376	34930605
No adverse event	221.08	20.13	152	21798	22775	34912206
Product physical issue	211.64	20.13	74	21876	2467	34932514

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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	737.37	19.14	517	28137	140788	79574946
Diarrhoea	705.64	19.14	1182	27472	879307	78836427
Pneumonia	550.45	19.14	904	27750	659342	79056392
Off label use	507.53	19.14	1045	27609	906170	78809564
Platelet count decreased	448.95	19.14	444	28210	194220	79521514
Thrombocytopenia	430.26	19.14	502	28152	264757	79450977
Death	335.58	19.14	670	27984	565844	79149890
Plasma cell myeloma recurrent	299.86	19.14	99	28555	4902	79710832
Plasma cell myeloma	247.53	19.14	182	28472	53077	79662657
Product physical issue	219.81	19.14	75	28579	4110	79711624

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XG03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Proteasome inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:52726	proteasome inhibitors
CHEBI has role	CHEBI:68495	Type I cell-death inducers
CHEBI has role	CHEBI:71031	orphan drugs
CHEBI has role	CHEBI:49103	drug metabolites
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|

Disease	Relation	SNOMED_ID	DOID
Multiple myeloma	indication	109989006	DOID:9538

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.27	acidic
pKa2	12.17	acidic
pKa3	13.45	acidic

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
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9233115	Aug. 12, 2024	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8003819	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8530694	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8871745	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9175017	June 16, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	7442830	Nov. 20, 2029	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	9233115	Aug. 12, 2024	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8003819	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8530694	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	8871745	Aug. 6, 2027	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

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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 beta type-5	Enzyme	P28074	PSB5_HUMAN	INHIBITOR	IC50	8.47	SCIENTIFIC LITERATURE	DRUG LABEL
Proteasome subunit beta type-1	Enzyme	P20618	PSB1_HUMAN	INHIBITOR	IC50	7.51	SCIENTIFIC LITERATURE
Proteasome subunit beta type-2	Enzyme	P49721	PSB2_HUMAN	INHIBITOR	IC50	5.46	SCIENTIFIC LITERATURE
ATP-dependent Clp protease proteolytic subunit	Enzyme		CLPP_STAA8		EC50	5.44	CHEMBL
NACHT, LRR and PYD domains-containing protein 3	Unclassified		NLRP3_MOUSE		IC50	6.70	CHEMBL

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External reference:

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ID	Source
016599	NDDF
016600	NDDF
1239908-20-3	SECONDARY_CAS_RN
1723734	RXNORM
237159	MMSL
25183872	PUBCHEM_CID
31293	MMSL
4035138	VANDF
6V8	PDB_CHEM_ID
71050168A2	UNII

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-078	CAPSULE	2.30 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-078	CAPSULE	2.30 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-079	CAPSULE	3 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-079	CAPSULE	3 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-080	CAPSULE	4 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-080	CAPSULE	4 mg	ORAL	NDA	29 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-230	CAPSULE	2.30 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-230	CAPSULE	2.30 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-230	CAPSULE	2.30 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-390	CAPSULE	3 mg	ORAL	NDA	33 sections

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