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:

Property	Value	Reference
Vd (Volume of distribution)	3.61 L/kg	Lombardo F, Berellini G, Obach RS
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
t_half (Half-life)	97 hours	Lombardo F, Berellini G, Obach RS

Approvals:

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

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
Diarrhoea	798.24	20.83	1051	18615	587425	49998033
Neuropathy peripheral	521.04	20.83	372	19294	96385	50489073
Death	488.80	20.83	614	19052	324765	50260693
Adverse event	267.11	20.83	182	19484	43581	50541877
Thrombocytopenia	264.27	20.83	285	19381	127388	50458070
Platelet count decreased	248.26	20.83	247	19419	100479	50484979
Pneumonia	216.49	20.83	462	19204	377939	50207519
Plasma cell myeloma recurrent	176.74	20.83	58	19608	2600	50582858
Plasma cell myeloma	167.07	20.83	120	19546	31202	50554256
Off label use	160.11	20.83	474	19192	473952	50111506
Product physical issue	138.51	20.83	55	19611	4277	50581181
Nausea	134.30	20.83	584	19082	704814	49880644
Constipation	129.85	20.83	247	19419	185461	50399997
White blood cell count decreased	123.75	20.83	187	19479	116535	50468923
No adverse event	120.99	20.83	102	19564	33476	50551982
Full blood count decreased	106.46	20.83	80	19586	22266	50563192
Cytopenia	101.41	20.83	55	19611	8720	50576738
Product dose omission issue	91.64	20.83	213	19453	183625	50401833
Laboratory test abnormal	90.88	20.83	74	19592	23134	50562324
Neutrophil count decreased	86.74	20.83	98	19568	45928	50539530
Vomiting	83.00	20.83	376	19290	460382	50125076
Adverse drug reaction	70.93	20.83	97	19569	55125	50530333
Fatigue	68.66	20.83	489	19177	707112	49878346
Influenza	58.64	20.83	116	19550	89422	50496036
Drug ineffective	57.00	20.83	149	19517	819184	49766274
Dehydration	48.80	20.83	150	19516	152299	50433159
Neutropenia	45.89	20.83	144	19522	147821	50437637
Plasmacytoma	45.47	20.83	21	19645	2364	50583094
Muscle spasms	44.40	20.83	128	19538	125425	50460033
Paraesthesia	43.90	20.83	124	19542	120119	50465339
Drug interaction	43.29	20.83	12	19654	199609	50385849
Rash	42.56	20.83	303	19363	437168	50148290
Asthenia	40.87	20.83	237	19429	318805	50266653
Monoclonal immunoglobulin present	40.69	20.83	14	19652	726	50584732
Body dysmorphic disorder	40.49	20.83	11	19655	254	50585204
Toxicity to various agents	40.44	20.83	16	19650	212483	50372975
Product packaging quantity issue	39.07	20.83	15	19651	1065	50584393
Accidental exposure to product	38.24	20.83	46	19620	23011	50562447
Condition aggravated	37.65	20.83	36	19630	297022	50288436
COVID-19	37.46	20.83	66	19600	46596	50538862
Illness	35.95	20.83	46	19620	24494	50560964
Product blister packaging issue	35.90	20.83	9	19657	150	50585308
Light chain analysis increased	35.30	20.83	14	19652	1084	50584374
Treatment failure	34.42	20.83	6	19660	137631	50447827
Arthralgia	34.13	20.83	75	19591	438627	50146831
Glossodynia	33.84	20.83	3	19663	115566	50469892
Infusion related reaction	33.53	20.83	12	19654	169545	50415913
Cardiac amyloidosis	33.21	20.83	12	19654	719	50584739
Peripheral swelling	33.16	20.83	163	19503	205773	50379685
Cataract	33.04	20.83	63	19603	47237	50538221
Pain	32.44	20.83	116	19550	578787	50006671
Injection site pain	32.19	20.83	3	19663	111021	50474437
Therapeutic product effect decreased	31.77	20.83	7	19659	136043	50449415
COVID-19 pneumonia	31.24	20.83	26	19640	8369	50577089
Vitiligo	31.22	20.83	13	19653	1141	50584317
Drug hypersensitivity	31.12	20.83	31	19635	250979	50334479
Hepatic enzyme increased	30.26	20.83	8	19658	137372	50448086
Product packaging issue	29.94	20.83	12	19654	955	50584503
Joint ankylosis	29.04	20.83	11	19655	753	50584705
Monoclonal immunoglobulin increased	28.93	20.83	7	19659	100	50585358
Discomfort	28.74	20.83	4	19662	108376	50477082
Wound	27.83	20.83	4	19662	105790	50479668
Decreased appetite	27.47	20.83	152	19514	200771	50384687
Back pain	27.17	20.83	162	19504	219868	50365590
VIth nerve paresis	25.25	20.83	6	19660	79	50585379
Blood potassium decreased	24.32	20.83	48	19618	36897	50548561
Product use issue	24.22	20.83	14	19652	149461	50435997
Ageusia	24.11	20.83	26	19640	11557	50573901
Musculoskeletal stiffness	23.89	20.83	10	19656	128471	50456987
Hypoglossal nerve paresis	23.60	20.83	6	19660	106	50585352
Blood immunoglobulin G increased	23.12	20.83	11	19655	1324	50584134
Headache	23.03	20.83	110	19556	506425	50079033
Eye swelling	22.32	20.83	33	19633	20111	50565347
Product packaging difficult to open	22.03	20.83	5	19661	53	50585405
Haemorrhoidal haemorrhage	21.74	20.83	15	19651	3652	50581806
Tumour lysis syndrome	21.62	20.83	20	19646	7401	50578057
Tachycardia	21.60	20.83	6	19660	99757	50485701
Product use in unapproved indication	21.56	20.83	9	19657	115810	50469648
Hypertension	20.96	20.83	31	19635	211172	50374286

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
Death	491.83	20.83	802	17375	341282	29215068
Neuropathy peripheral	443.83	20.83	359	17818	70668	29485682
Pneumonia	299.20	20.83	625	17552	319547	29236803
Adverse event	283.83	20.83	153	18024	15138	29541212
Diarrhoea	271.41	20.83	615	17562	332083	29224267
Off label use	234.91	20.83	547	17630	300253	29256097
Platelet count decreased	184.23	20.83	271	17906	104401	29451949
No adverse event	183.09	20.83	121	18056	17357	29538993
Thrombocytopenia	175.37	20.83	304	17873	134519	29421831
Plasma cell myeloma recurrent	162.36	20.83	67	18110	3616	29552734
Plasma cell myeloma	161.47	20.83	153	18024	36962	29519388
Product physical issue	156.82	20.83	56	18121	2032	29554318
Full blood count decreased	153.79	20.83	105	18072	15887	29540463
Laboratory test abnormal	119.67	20.83	95	18082	18090	29538260
Fatigue	109.34	20.83	433	17744	316388	29239962
Constipation	108.01	20.83	225	17952	113935	29442415
Rash	106.73	20.83	306	17871	189513	29366837
Drug interaction	104.05	20.83	4	18173	197381	29358969
Adverse drug reaction	94.95	20.83	94	18083	23926	29532424
White blood cell count decreased	91.62	20.83	175	18002	83187	29473163
Influenza	83.10	20.83	115	18062	41766	29514584
Peripheral swelling	81.63	20.83	143	18034	63596	29492754
Product dose omission issue	80.81	20.83	181	17996	96202	29460148
Light chain analysis increased	80.68	20.83	29	18148	1072	29555278
Toxicity to various agents	66.61	20.83	13	18164	173648	29382702
COVID-19	61.34	20.83	92	18085	35922	29520428
Cytopenia	53.35	20.83	46	18131	9813	29546537
Accidental exposure to product	51.86	20.83	47	18130	10706	29545644
Back pain	50.73	20.83	158	18019	102126	29454224
Thrombosis	41.94	20.83	86	18091	42959	29513391
Monoclonal immunoglobulin present	41.85	20.83	17	18160	880	29555470
Product packaging issue	38.55	20.83	14	18163	533	29555817
Muscle spasms	38.41	20.83	107	18070	64975	29491375
Product blister packaging issue	37.72	20.83	9	18168	73	29556277
Product use in unapproved indication	36.62	20.83	5	18172	86870	29469480
Lower respiratory tract infection	35.89	20.83	61	18116	26441	29529909
Product packaging quantity issue	33.99	20.83	14	18163	751	29555599
Full blood count increased	33.48	20.83	14	18163	780	29555570
Tachycardia	30.91	20.83	4	18173	72406	29483944
Nausea	30.53	20.83	291	17886	288964	29267386
Neutropenia	29.45	20.83	159	18018	131552	29424798
Nasopharyngitis	29.38	20.83	92	18085	59573	29496777
Morganella infection	29.31	20.83	11	18166	460	29555890
Hypertension	27.52	20.83	19	18158	116595	29439755
Cryptosporidiosis infection	26.90	20.83	10	18167	407	29555943
Rhabdomyolysis	26.84	20.83	3	18174	60805	29495545
Asthenia	26.49	20.83	224	17953	215026	29341324
Illness	26.13	20.83	26	18151	6648	29549702
Condition aggravated	26	20.83	31	18146	146264	29410086
Bronchial haemorrhage	25.35	20.83	11	18166	672	29555678
Unevaluable event	24.88	20.83	56	18121	29795	29526555
JC virus CSF test positive	24.66	20.83	7	18170	118	29556232
Light chain disease	24.45	20.83	7	18170	122	29556228
Chillblains	24.36	20.83	5	18172	18	29556332
Laryngeal cancer metastatic	24.11	20.83	6	18171	59	29556291
Insomnia	23.94	20.83	113	18064	88648	29467702
Hypotension	23.51	20.83	53	18124	194301	29362049
Cataract	23.32	20.83	46	18131	22332	29534018
Spinal pain	22.94	20.83	21	18156	4843	29551507
Immunoglobulins decreased	21.84	20.83	10	18167	694	29555656
Plasmacytoma	21.57	20.83	17	18160	3198	29553152
Otitis externa bacterial	21.19	20.83	4	18173	8	29556342
Pneumonia influenzal	21.06	20.83	12	18165	1318	29555032
Seizure	20.89	20.83	16	18161	93107	29463243

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
Diarrhoea	600.76	19.91	971	21573	721733	63754455
Neuropathy peripheral	565.84	19.91	405	22139	117120	64359068
Pneumonia	517.85	19.91	791	21753	558785	63917403
Platelet count decreased	376.21	19.91	372	22172	167339	64308849
Off label use	359.00	19.91	722	21822	632084	63844104
Thrombocytopenia	330.01	19.91	398	22146	223403	64252785
Death	284.00	19.91	560	21984	482145	63994043
Plasma cell myeloma recurrent	220.05	19.91	74	22470	3991	64472197
Plasma cell myeloma	219.35	19.91	158	22386	45917	64430271
Product physical issue	160.23	19.91	56	22488	3393	64472795
No adverse event	152.26	19.91	105	22439	28456	64447732
White blood cell count decreased	145.69	19.91	224	22320	157613	64318575
Neutrophil count decreased	122.76	19.91	143	22401	77053	64399135
Product dose omission issue	121.15	19.91	232	22312	194515	64281673
Full blood count decreased	117.96	19.91	82	22462	22500	64453688
Rash	112.92	19.91	384	22160	458165	64018023
Constipation	98.45	19.91	235	22309	229102	64247086
Influenza	95.13	19.91	149	22395	106382	64369806
Drug interaction	84.26	19.91	13	22531	362070	64114118
Toxicity to various agents	74.15	19.91	18	22526	363495	64112693
Fatigue	72.71	19.91	478	22066	748252	63727936
Cytopenia	71.16	19.91	52	22492	15419	64460769
Nausea	71.13	19.91	493	22051	785307	63690881
Laboratory test abnormal	60.54	19.91	57	22487	24006	64452182
COVID-19	59.35	19.91	92	22452	65048	64411140
Product blister packaging issue	52.79	19.91	12	22532	144	64476044
Light chain analysis increased	52.28	19.91	19	22525	1289	64474899
Plasmacytoma	52.22	19.91	26	22518	3844	64472344
Dehydration	51.77	19.91	180	22364	216583	64259605
Product packaging quantity issue	46.08	19.91	16	22528	950	64475238
Drug ineffective	41.36	19.91	153	22391	840094	63636094
Pain	41.36	19.91	82	22462	553429	63922759
Neutropenia	39.39	19.91	177	22367	239447	64236741
Product packaging issue	38.29	19.91	14	22530	966	64475222
Body dysmorphic disorder	37.14	19.91	10	22534	249	64475939
Cardiac amyloidosis	36.68	19.91	15	22529	1400	64474788
Peripheral swelling	36.27	19.91	157	22387	208996	64267192
Accidental exposure to product	35.61	19.91	45	22499	26319	64449869
Vomiting	34.90	19.91	319	22225	550798	63925390
Hypertension	34.83	19.91	24	22520	259237	64216951
Anaemia	33.08	19.91	236	22308	378444	64097744
Adverse drug reaction	33.02	19.91	58	22486	45406	64430782
Drug hypersensitivity	31.96	19.91	22	22522	237793	64238395
Product use in unapproved indication	31.82	19.91	11	22533	176607	64299581
Muscle spasms	31.81	19.91	115	22429	140908	64335280
Headache	31.12	19.91	89	22455	529378	63946810
COVID-19 pneumonia	30.34	19.91	33	22511	16471	64459717
Hypotension	29.66	19.91	55	22489	380919	64095269
Tachycardia	29.31	19.91	8	22536	149571	64326617
Sepsis	29.17	19.91	158	22386	230183	64246005
Monoclonal immunoglobulin present	29.09	19.91	11	22533	834	64475354
Arthralgia	28.50	19.91	71	22473	442189	64033999
Pneumonia influenzal	28.40	19.91	15	22529	2507	64473681
Injection site pain	28.28	19.91	3	22541	111405	64364783
Cryptosporidiosis infection	28.12	19.91	10	22534	637	64475551
Asthenia	27.68	19.91	249	22295	427795	64048393
Musculoskeletal stiffness	27.33	19.91	5	22539	123201	64352987
Full blood count increased	27.31	19.91	9	22535	455	64475733
Vitiligo	27.22	19.91	13	22531	1755	64474433
Condition aggravated	27.06	19.91	56	22488	372370	64103818
Taste disorder	26.95	19.91	24	22520	9409	64466779
Cataract	26.92	19.91	57	22487	51205	64424983
JC virus CSF test positive	26.87	19.91	7	22537	153	64476035
Joint ankylosis	26.44	19.91	10	22534	759	64475429
Back pain	26.08	19.91	163	22381	250008	64226180
Hypercalcaemia	25.35	19.91	42	22502	31374	64444814
Upper respiratory tract inflammation	25.22	19.91	16	22528	3766	64472422
Light chain disease	24.82	19.91	7	22537	208	64475980
Herpes zoster	24.56	19.91	72	22472	79115	64397073
Immunoglobulins decreased	24.37	19.91	11	22533	1307	64474881
Cardiac failure	24.18	19.91	101	22443	132272	64343916
Hypoglossal nerve paresis	24.08	19.91	6	22538	109	64476079
Squamous cell carcinoma of skin	24.05	19.91	25	22519	11851	64464337
Morganella infection	23.83	19.91	10	22534	996	64475192
Nasopharyngitis	23.81	19.91	133	22411	195940	64280248
Treatment failure	23.35	19.91	6	22538	116810	64359378
Therapeutic product effect decreased	22.91	19.91	6	22538	115345	64360843
Laryngeal cancer metastatic	22.83	19.91	5	22539	50	64476138
VIth nerve paresis	22.82	19.91	6	22538	136	64476052
Infusion related reaction	22.37	19.91	15	22529	164452	64311736
Bronchial haemorrhage	21.96	19.91	10	22534	1212	64474976
Blood calcium abnormal	21.72	19.91	10	22534	1244	64474944
Blood immunoglobulin G increased	20.87	19.91	11	22533	1830	64474358
Polyneuropathy	20.82	19.91	30	22514	19864	64456324
Blood pressure increased	20.59	19.91	18	22526	172534	64303654
Hepatic enzyme increased	20.31	19.91	10	22534	129933	64346255

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XG03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Proteasome inhibitors
FDA MoA	N0000175075	Proteasome Inhibitors
FDA EPC	N0000175604	Proteasome Inhibitor
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D011480	Protease 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

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)

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 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 4MG 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 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
EQ 4MG 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 4MG 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 4MG 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 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 4MG 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	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 4MG 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

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 2.3MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	Nov. 20, 2022	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	Nov. 20, 2022	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE	NINLARO	TAKEDA PHARMS USA	N208462	Nov. 20, 2015	RX	CAPSULE	ORAL	Nov. 20, 2022	USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

Bioactivity Summary:

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

External reference:

ID	Source
71050168A2	UNII
D10130	KEGG_DRUG
1239908-20-3	SECONDARY_CAS_RN
4035138	VANDF
C3273711	UMLSCUI
CHEBI:90942	CHEBI
6V8	PDB_CHEM_ID
CHEMBL2141296	ChEMBL_ID
25183872	PUBCHEM_CID
DB09570	DRUGBANK_ID
CHEMBL3545432	ChEMBL_ID
CHEMBL1813256	ChEMBL_ID
9411	INN_ID
C548400	MESH_SUPPLEMENTAL_RECORD_UI
C000595706	MESH_SUPPLEMENTAL_RECORD_UI
8450	IUPHAR_LIGAND_ID
1723734	RXNORM
237159	MMSL
31293	MMSL
d08398	MMSL
715256005	SNOMEDCT_US
781324002	SNOMEDCT_US
784168005	SNOMEDCT_US
016599	NDDF
016600	NDDF

Pharmaceutical products:

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	63020-079	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	63020-230	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
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-390	CAPSULE	3 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-400	CAPSULE	4 mg	ORAL	NDA	33 sections
NINLARO	HUMAN PRESCRIPTION DRUG LABEL	1	63020-400	CAPSULE	4 mg	ORAL	NDA	33 sections