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

Stem definition	Drug id	CAS RN
humanized origin	5362	909395-70-6

Description:

Molecule	Description
Synonyms: romosozumab romosozumab-aqqg evenity AMG 785 AMG-785 anti-sclerostin monoclonal antibody CDP-7851 sclerostin Ab	Romosozumab-aqqg is a humanized monoclonal antibody (IgG2) produced in a mammalian cell line (Chinese Hamster Ovary) by recombinant DNA technology that binds to and inhibits the action of sclerostin, a regulatory factor in bone metabolism. Romosozumab increases bone formation and, to a lesser extent, decreases bone resorption. Animal studies showed that romosozumab-aqqg stimulates new bone formation on trabecular and cortical bone surfaces by stimulating osteoblastic activity resulting in increases in trabecular and cortical bone mass and improvements in bone structure and strength. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

romosozumab
romosozumab-aqqg
evenity
AMG 785
AMG-785
anti-sclerostin monoclonal antibody
CDP-7851
sclerostin Ab

Romosozumab-aqqg is a humanized monoclonal antibody (IgG2) produced in a mammalian cell line (Chinese Hamster Ovary) by recombinant DNA technology that binds to and inhibits the action of sclerostin, a regulatory factor in bone metabolism. Romosozumab increases bone formation and, to a lesser extent, decreases bone resorption. Animal studies showed that romosozumab-aqqg stimulates new bone formation on trabecular and cortical bone surfaces by stimulating osteoblastic activity resulting in increases in trabecular and cortical bone mass and improvements in bone structure and strength.

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

Dose	Unit	Route
7	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company
Dec. 9, 2019	EMA	UCB PHARMA S.A.
April 9, 2019	FDA	AMGEN INC
Aug. 1, 2019	PMDA	AMGEN ASTELLAS BIOPHARMA K.K.

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
Fall	418.52	23.83	340	6483	391994	63090205
Fracture	332.14	23.83	111	6712	19473	63462726
Injection site pain	283.51	23.83	175	6648	129625	63352574
Spinal compression fracture	230.37	23.83	78	6745	14205	63467994
Spinal fracture	207.90	23.83	77	6746	18194	63464005
Femoral neck fracture	196.30	23.83	61	6762	8462	63473737
Femur fracture	190.94	23.83	92	6731	41664	63440535
Injection site swelling	182.47	23.83	93	6730	47479	63434720
Injection site erythema	153.46	23.83	101	6722	83073	63399126
Bone density decreased	124.78	23.83	50	6773	14562	63467637
Cardiac failure	119.42	23.83	89	6734	89053	63393146
Bone pain	102.26	23.83	67	6756	54574	63427625
Compression fracture	95.26	23.83	33	6790	6415	63475784
Radius fracture	92.07	23.83	28	6795	3607	63478592
Thoracic vertebral fracture	89.69	23.83	29	6794	4563	63477636
Cerebral infarction	78.06	23.83	42	6781	23851	63458348
Lumbar vertebral fracture	75.38	23.83	27	6796	5783	63476416
Pathological fracture	74.61	23.83	30	6793	8804	63473395
Renal impairment	71.70	23.83	66	6757	88289	63393910
Transient ischaemic attack	69.88	23.83	46	6777	37707	63444492
Injury associated with device	66.92	23.83	22	6801	3644	63478555
Aortic dissection	66.23	23.83	19	6804	1999	63480200
Physical deconditioning	61.64	23.83	15	6808	834	63481365
Injection site mass	61.51	23.83	33	6790	18623	63463576
Myocardial infarction	55.90	23.83	61	6762	99832	63382367
Arrhythmia	53.05	23.83	39	6784	38101	63444098
Marasmus	52.39	23.83	12	6811	513	63481686
Injection site induration	50.34	23.83	23	6800	9203	63472996
Wrong product administered	48.91	23.83	20	6803	6121	63476078
Humerus fracture	47.93	23.83	22	6801	8894	63473305
Angina pectoris	46.97	23.83	33	6790	30045	63452154
Osteonecrosis of jaw	46.79	23.83	35	6788	35088	63447111
Injection site pruritus	45.17	23.83	38	6785	45078	63437121
Pelvic fracture	45.09	23.83	24	6799	13324	63468875
Arthralgia	43.53	23.83	147	6676	569563	62912636
Hip fracture	42.94	23.83	31	6792	29443	63452756
Blood parathyroid hormone increased	42.75	23.83	15	6808	3023	63479176
Occupational exposure to product	40.07	23.83	13	6810	2065	63480134
Myalgia	38.87	23.83	62	6761	146467	63335732
Wrist fracture	36.47	23.83	21	6802	13566	63468633
Injection site rash	34.98	23.83	23	6800	18786	63463413
Injection site reaction	34.93	23.83	37	6786	58487	63423712
Hospitalisation	34.36	23.83	44	6779	85037	63397162
Cerebrovascular accident	33.27	23.83	49	6774	107975	63374224
Pseudarthrosis	32.76	23.83	8	6815	451	63481748
Upper limb fracture	30.04	23.83	21	6802	18947	63463252
Tartrate-resistant acid phosphatase increased	29.78	23.83	4	6819	4	63482195
Injection site warmth	29.28	23.83	19	6804	15176	63467023
Cerebral haemorrhage	28.94	23.83	25	6798	30704	63451495
Hypocalcaemia	28.26	23.83	25	6798	31688	63450511
Blood calcium decreased	27.96	23.83	23	6800	26428	63455771
Dementia	27.90	23.83	20	6803	18774	63463425
Death	25.36	23.83	93	6730	374288	63107911
Blood alkaline phosphatase increased	25.34	23.83	27	6796	42940	63439259
Ulna fracture	25.30	23.83	8	6815	1170	63481029
Diarrhoea	23.99	23.83	25	6798	715341	62766858

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
Off label use	124.53	69.46	68	320	419456	34537087

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
Fall	311.75	25.19	247	4591	487382	79252168
Spinal compression fracture	177.22	25.19	58	4780	16900	79722650
Femoral neck fracture	167.11	25.19	49	4789	9935	79729615
Injection site pain	147.71	25.19	94	4744	129744	79609806
Femur fracture	140.48	25.19	61	4777	38591	79700959
Injection site swelling	128.89	25.19	61	4777	47071	79692479
Spinal fracture	127.23	25.19	46	4792	18008	79721542
Cardiac failure	107.80	25.19	83	4755	154759	79584791
Radius fracture	103.63	25.19	27	4811	3537	79736013
Injection site erythema	92.24	25.19	58	4780	78139	79661411
Fracture	84.39	25.19	36	4802	21765	79717785
Cerebral infarction	69.70	25.19	40	4798	45636	79693914
Bone density decreased	68.57	25.19	27	4811	13320	79726230
Thoracic vertebral fracture	67.31	25.19	21	4817	5232	79734318
Lumbar vertebral fracture	57.45	25.19	20	4818	7002	79732548
Aortic dissection	54.79	25.19	17	4821	4158	79735392
Marasmus	51.19	25.19	12	4826	1016	79738534
Bone pain	50.28	25.19	35	4803	55707	79683843
Injection site induration	47.42	25.19	19	4819	9800	79729750
Transient ischaemic attack	47.32	25.19	33	4805	52662	79686888
Renal impairment	45.76	25.19	52	4786	157731	79581819
Injection site mass	45.73	25.19	23	4815	20161	79719389
Osteonecrosis of jaw	41.00	25.19	28	4810	43198	79696352
Compression fracture	40.09	25.19	15	4823	6445	79733105
Humerus fracture	34.77	25.19	15	4823	9298	79730252
Arthralgia	34.76	25.19	94	4744	571709	79167841
Angina pectoris	34.30	25.19	27	4811	51705	79687845
Myocardial infarction	33.29	25.19	48	4790	184081	79555469
Tartrate-resistant acid phosphatase increased	31.18	25.19	4	4834	6	79739544
Pelvic fracture	30.89	25.19	15	4823	12189	79727361
Pseudarthrosis	28.85	25.19	6	4832	292	79739258
Wrist fracture	28.23	25.19	14	4824	11907	79727643
Injection site pruritus	27.88	25.19	22	4816	42261	79697289
Cerebral haemorrhage	27.71	25.19	25	4813	57648	79681902
Blood calcium decreased	26.41	25.19	19	4819	31800	79707750
Injection site rash	25.45	25.19	15	4823	17939	79721611
Physical deconditioning	25.37	25.19	8	4830	2062	79737488
Ulna fracture	25.36	25.19	7	4831	1138	79738412

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	M05BX06	MUSCULO-SKELETAL SYSTEM DRUGS FOR TREATMENT OF BONE DISEASES DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION Other drugs affecting bone structure and mineralization

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

Disease	Relation	SNOMED_ID	DOID
Postmenopausal osteoporosis	indication	102447009
Hypocalcemia	contraindication	5291005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Sclerostin	Glycoprotein	Q9BQB4	SOST_HUMAN	BINDING AGENT	Kd	11.70		IUPHAR	DRUG LABEL

External reference:

ID	Source
CHEMBL2107874	ChEMBL_ID
D10156	KEGG_DRUG
C557282	MESH_SUPPLEMENTAL_RECORD_UI
8092	IUPHAR_LIGAND_ID
DB11866	DRUGBANK_ID
017957	NDDF
787359005	SNOMEDCT_US
787415000	SNOMEDCT_US
4038317	VANDF
C3661283	UMLSCUI
9533	INN_ID
2123126	RXNORM
313417	MMSL
36679	MMSL
d09226	MMSL
3VHF2ZD92J	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Evenity	HUMAN PRESCRIPTION DRUG LABEL	1	55513-880	INJECTION, SOLUTION	105 mg	SUBCUTANEOUS	BLA	28 sections
Evenity	HUMAN PRESCRIPTION DRUG LABEL	1	55513-880	INJECTION, SOLUTION	105 mg	SUBCUTANEOUS	BLA	28 sections