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

Stem definition	Drug id	CAS RN
human origin	5234	1428935-60-7

Description:

Molecule	Description
Synonyms: durvalumab MEDI4736 MEDI 4736 imfinzi durvalumab (genetical recombination)	Durvalumab is a human immunoglobulin G1 kappa (IgG1κ) monoclonal antibody that blocks the interaction of PD-L1 with PD-1 and CD80 (B7.1). Blockade of PD-L1/PD-1 and PD-L1/CD80 interactions releases the inhibition of immune responses, without inducing antibody dependent cellmediated cytotoxicity (ADCC). PD-L1 blockade with durvalumab led to increased T-cell activation in vitro and decreased tumor size in co-engrafted human tumor and immune cell xenograft mouse models. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

durvalumab
MEDI4736
MEDI 4736
imfinzi
durvalumab (genetical recombination)

Durvalumab is a human immunoglobulin G1 kappa (IgG1κ) monoclonal antibody that blocks the interaction of PD-L1 with PD-1 and CD80 (B7.1). Blockade of PD-L1/PD-1 and PD-L1/CD80 interactions releases the inhibition of immune responses, without inducing antibody dependent cellmediated cytotoxicity (ADCC). PD-L1 blockade with durvalumab led to increased T-cell activation in vitro and decreased tumor size in co-engrafted human tumor and immune cell xenograft mouse models.

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

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
Sept. 21, 2018	EMA	ASTRAZENECA AB
May 1, 2017	FDA	ASTRAZENECA UK LTD
July 2, 2018	PMDA	AstraZeneca KK

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
Radiation pneumonitis	605.83	37.26	102	3916	1481	63483523
Malignant neoplasm progression	328.58	37.26	140	3878	81981	63403023
Pneumonitis	322.57	37.26	110	3908	35112	63449892
Biliary tract infection	191.96	37.26	34	3984	668	63484336
Death	123.41	37.26	134	3884	374247	63110757
Metastases to central nervous system	108.34	37.26	38	3980	13067	63471937
Pyrexia	97.18	37.26	133	3885	470345	63014659
Drug-induced liver injury	95.77	37.26	48	3970	40174	63444830
Pemphigoid	91.44	37.26	29	3989	7315	63477689
Febrile neutropenia	89.90	37.26	68	3950	118381	63366623
Cholangitis infective	88.66	37.26	16	4002	350	63484654
Urinary tract obstruction	74.52	37.26	19	3999	2189	63482815
Colitis	71.12	37.26	42	3976	48486	63436518
Tumour hyperprogression	70.14	37.26	11	4007	98	63484906
Embolism	69.46	37.26	24	3994	7882	63477122
Bile duct stenosis	63.71	37.26	15	4003	1241	63483763
Small intestinal obstruction	59.21	37.26	27	3991	18310	63466694
Neutrophil count decreased	57.98	37.26	39	3979	56367	63428637
Interstitial lung disease	52.40	37.26	38	3980	61870	63423134
Myocarditis	49.13	37.26	20	3998	10305	63474699
Bacillus infection	47.56	37.26	11	4007	842	63484162
Immune-mediated hepatitis	47.26	37.26	12	4006	1359	63483645
Hypothyroidism	45.05	37.26	30	3988	42602	63442402
Myasthenia gravis	44.51	37.26	15	4003	4566	63480438
Immune-mediated enterocolitis	42.13	37.26	12	4006	2099	63482905
Skin toxicity	40.20	37.26	14	4004	4700	63480304
Nephritis	40.05	37.26	12	4006	2504	63482500
Autoimmune nephritis	37.65	37.26	8	4010	414	63484590

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
Radiation pneumonitis	2129.81	24.41	384	7117	2256	34947174
Pneumonitis	692.45	24.41	263	7238	33615	34915815
Malignant neoplasm progression	517.60	24.41	287	7214	87759	34861671
Interstitial lung disease	290.32	24.41	178	7323	65104	34884326
Metastases to central nervous system	204.75	24.41	74	7427	8131	34941299
Neutrophil count decreased	186.15	24.41	123	7378	50981	34898449
Death	171.91	24.41	305	7196	397744	34551686
Immune-mediated hepatitis	124.69	24.41	37	7464	2178	34947252
Myelosuppression	124.03	24.41	67	7434	19198	34930232
Non-small cell lung cancer recurrent	119.70	24.41	18	7483	22	34949408
Myocarditis	103.45	24.41	53	7448	13629	34935801
Febrile neutropenia	99.52	24.41	134	7367	136715	34812715
Colitis	98.09	24.41	74	7427	37676	34911754
Lung disorder	94.57	24.41	70	7431	34626	34914804
Immune-mediated lung disease	87.04	24.41	26	7475	1565	34947865
Biliary tract infection	79.33	24.41	20	7481	635	34948795
Hypothyroidism	77.61	24.41	51	7450	20851	34928579
Drug-induced liver injury	67.17	24.41	53	7448	28779	34920651
Pulmonary toxicity	61.99	24.41	29	7472	6118	34943312
Enterocolitis infectious	60.53	24.41	20	7481	1675	34947755
Pneumonia	59.19	24.41	191	7310	362436	34586994
Myositis	53.63	24.41	33	7468	12037	34937393
Pneumothorax	44.24	24.41	35	7466	19057	34930373
Hepatic function abnormal	44.24	24.41	51	7450	44312	34905118
Pleural effusion	43.35	24.41	69	7432	81477	34867953
Pulmonary radiation injury	42.71	24.41	8	7493	58	34949372
Hyperthyroidism	39.73	24.41	26	7475	10540	34938890
Hypophysitis	36.81	24.41	15	7486	2271	34947159
Metastases to bone	34.49	24.41	25	7476	11945	34937485
Liver function test increased	34.38	24.41	27	7474	14538	34934892
Tumour hyperprogression	34.04	24.41	7	7494	86	34949344
Myasthenia gravis	33.46	24.41	20	7481	6920	34942510
Diffuse uveal melanocytic proliferation	33.30	24.41	5	7496	6	34949424
Adrenal insufficiency	33.07	24.41	26	7475	14021	34935409
Metastases to adrenals	32.40	24.41	11	7490	1001	34948429
Immune thrombocytopenia	30.75	24.41	21	7480	9131	34940299
Haemoptysis	29.57	24.41	37	7464	34969	34914461
Eastern Cooperative Oncology Group performance status worsened	28.56	24.41	10	7491	998	34948432
Enterocolitis	28.36	24.41	19	7482	8007	34941423
Oropharyngeal oedema	27.82	24.41	6	7495	94	34949336
Radiation oesophagitis	27.60	24.41	8	7493	433	34948997
Metastases to lymph nodes	26.43	24.41	15	7486	4713	34944717
Pneumonia bacterial	25.87	24.41	21	7480	11851	34937579
Platelet count decreased	24.99	24.41	69	7432	119648	34829782

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
Radiation pneumonitis	2748.85	27.60	472	10184	3461	79730271
Pneumonitis	758.36	27.60	290	10366	60570	79673162
Malignant neoplasm progression	632.01	27.60	324	10332	135666	79598066
Interstitial lung disease	360.40	27.60	210	10446	112390	79621342
Biliary tract infection	252.71	27.60	54	10602	1334	79732398
Neutrophil count decreased	243.03	27.60	153	10503	93806	79639926
Metastases to central nervous system	224.92	27.60	84	10572	16291	79717441
Death	187.01	27.60	297	10359	566217	79167515
Febrile neutropenia	181.88	27.60	187	10469	230812	79502920
Colitis	173.63	27.60	113	10543	73194	79660538
Myelosuppression	160.76	27.60	87	10569	40209	79693523
Immune-mediated hepatitis	159.12	27.60	45	10611	3611	79730121
Drug-induced liver injury	151.87	27.60	100	10556	66017	79667715
Myocarditis	127.79	27.60	61	10595	21672	79712060
Non-small cell lung cancer recurrent	121.32	27.60	20	10636	108	79733624
Immune-mediated lung disease	112.51	27.60	31	10625	2259	79731473
Hypothyroidism	110.08	27.60	75	10581	52317	79681415
Pyrexia	90.30	27.60	245	10411	678464	79055268
Hepatic function abnormal	83.78	27.60	73	10583	73034	79660698
Pleural effusion	78.76	27.60	97	10559	145165	79588567
Lung disorder	75.77	27.60	72	10584	80485	79653247
Pemphigoid	75.12	27.60	38	10618	15277	79718455
Pneumonia	74.76	27.60	225	10431	660021	79073711
Tumour hyperprogression	73.28	27.60	14	10642	192	79733540
Myasthenia gravis	72.96	27.60	33	10623	10366	79723366
Platelet count decreased	70.65	27.60	107	10549	194557	79539175
Radiation interaction	67.43	27.60	11	10645	55	79733677
Cholangitis infective	66.91	27.60	16	10640	661	79733071
Bile duct stenosis	66.43	27.60	20	10636	1996	79731736
Pulmonary toxicity	66.15	27.60	33	10623	12881	79720851
Embolism	63.67	27.60	33	10623	13949	79719783
Myositis	56.53	27.60	34	10622	19134	79714598
Hypophysitis	55.81	27.60	21	10635	4145	79729587
Metastases to bone	53.73	27.60	36	10620	24391	79709341
Pneumothorax	53.49	27.60	38	10618	28285	79705447
Adrenal insufficiency	53.29	27.60	38	10618	28449	79705283
Pulmonary radiation injury	52.84	27.60	9	10647	61	79733671
Hyperthyroidism	51.92	27.60	34	10622	22175	79711557
Pain	50.00	27.60	16	10640	703786	79029946
Thyroiditis	46.80	27.60	19	10637	4586	79729146
Cholangitis	46.54	27.60	26	10630	12750	79720982
Hepatic infection	46.15	27.60	13	10643	1027	79732705
Immune-mediated enterocolitis	45.93	27.60	19	10637	4811	79728921
Encephalitis autoimmune	43.67	27.60	15	10641	2279	79731453
Small intestinal obstruction	41.21	27.60	32	10624	27240	79706492
Diabetic ketoacidosis	40.94	27.60	35	10621	34087	79699645
Enterocolitis infectious	40.40	27.60	15	10641	2854	79730878
Urinary tract obstruction	39.49	27.60	17	10639	4748	79728984
Respiratory failure	38.86	27.60	79	10577	180832	79552900
Headache	38.09	27.60	20	10636	653752	79079980
Drug ineffective	37.70	27.60	54	10602	1080859	78652873
Sepsis	36.32	27.60	98	10558	269330	79464402
Immune thrombocytopenia	36.21	27.60	25	10631	17780	79715952
Bacillus infection	36.09	27.60	11	10645	1144	79732588
Superior vena cava syndrome	35.24	27.60	11	10645	1238	79732494
Metastases to adrenals	34.56	27.60	11	10645	1319	79732413
Pericardial effusion	33.67	27.60	36	10620	46201	79687531
Eastern Cooperative Oncology Group performance status worsened	33.55	27.60	12	10644	2053	79731679
Liver function test increased	32.61	27.60	33	10623	39740	79693992
Radiation oesophagitis	32.31	27.60	9	10647	682	79733050
Autoimmune nephritis	31.71	27.60	9	10647	730	79733002
Metastases to lung	31.17	27.60	23	10633	18140	79715592
Lipase increased	30.87	27.60	22	10634	16444	79717288
Limbic encephalitis	30.21	27.60	9	10647	866	79732866
Thrombocytopenia	29.45	27.60	90	10566	265169	79468563
Organising pneumonia	28.67	27.60	18	10638	10921	79722811
Nephritis	28.38	27.60	13	10643	4201	79729531
Presyncope	28.20	27.60	31	10625	41023	79692709
Haemoptysis	28.07	27.60	36	10620	55963	79677769
Joint swelling	27.97	27.60	3	10653	288643	79445089
Hypopituitarism	27.75	27.60	12	10644	3387	79730345
Pneumonia bacterial	27.73	27.60	22	10634	19309	79714423
Diffuse uveal melanocytic proliferation	27.64	27.60	4	10652	7	79733725

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01FF03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES PD-1/PDL-1 (Programmed cell death protein 1/death ligand 1) inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D000074322	Antineoplastic Agents, Immunological
FDA CS	M0001357	Antibodies, Monoclonal
FDA MoA	N0000193336	Programmed Death Ligand-1-directed Antibody Interactions
FDA MoA	N0000193337	Programmed Death Ligand-1 Antagonists
FDA EPC	N0000193338	Programmed Death Ligand-1 Blocker

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

Disease	Relation	SNOMED_ID	DOID
Transitional cell carcinoma	indication	27090000	DOID:2671
Liver cell carcinoma	indication	109841003	DOID:684
Small cell carcinoma of lung	indication	254632001	DOID:5409
Non-small cell lung cancer	indication	254637007	DOID:3908
Extensive stage primary small cell carcinoma of lung	indication
Metastatic carcinoma to biliary tract	indication

🐶 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
Programmed cell death 1 ligand 1	CD molecules	Q9NZQ7	PD1L1_HUMAN	ANTIBODY BINDING				UNKNOWN	DRUG LABEL

External reference:

ID	Source
28X28X9OKV	UNII
4036653	VANDF
C4055109	UMLSCUI
CHEMBL3301587	ChEMBL_ID
DB11714	DRUGBANK_ID
D10808	KEGG_DRUG
10010	INN_ID
7985	IUPHAR_LIGAND_ID
256648	MMSL
32681	MMSL
d08576	MMSL
017200	NDDF
735230005	SNOMEDCT_US
763588004	SNOMEDCT_US
1919503	RXNORM
C000613593	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4500	INJECTION, SOLUTION	120 mg	INTRAVENOUS	BLA	25 sections
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4500	INJECTION, SOLUTION	120 mg	INTRAVENOUS	BLA	25 sections
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4500	INJECTION, SOLUTION	120 mg	INTRAVENOUS	BLA	25 sections
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4500	INJECTION, SOLUTION	120 mg	INTRAVENOUS	BLA	25 sections
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4611	INJECTION, SOLUTION	500 mg	INTRAVENOUS	BLA	25 sections
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4611	INJECTION, SOLUTION	500 mg	INTRAVENOUS	BLA	25 sections
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4611	INJECTION, SOLUTION	500 mg	INTRAVENOUS	BLA	25 sections
IMFINZI	HUMAN PRESCRIPTION DRUG LABEL	1	0310-4611	INJECTION, SOLUTION	500 mg	INTRAVENOUS	BLA	25 sections