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

Stem definition	Drug id	CAS RN
antineoplastic, alkylating agents, methanesulfonates	2718	299-75-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: treosulfan threosulphan treosulphan tresulfan trecondi	immunosuppressant; RN given refers to (S-(R,R))-isomer Molecular weight: 278.29 Formula: C6H14O8S2 CLOGP: -2.20 LIPINSKI: 0 HAC: 8 HDO: 2 TPSA: 127.20 ALOGS: -1.21 ROTB: 7

Molecule

Description

Molfile Inchi Smiles

Synonyms:

treosulfan
threosulphan
treosulphan
tresulfan
trecondi

immunosuppressant; RN given refers to (S-(R*,R*))-isomer

Molecular weight: 278.29
Formula: C6H14O8S2
CLOGP: -2.20
LIPINSKI: 0
HAC: 8
HDO: 2
TPSA: 127.20
ALOGS: -1.21
ROTB: 7

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	97 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.59 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	4.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.83 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
June 20, 2019	EMA	medac Gesellschaft fur klinische Spezialpraparate mbH

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
Adenovirus infection	204.67	87.80	40	1552	3531	63483899
Graft versus host disease in skin	169.24	87.80	33	1559	2872	63484558
Human herpesvirus 6 infection	162.55	87.80	32	1560	2925	63484505
Acute graft versus host disease in skin	157.61	87.80	32	1560	3420	63484010
Cytomegalovirus infection reactivation	135.97	87.80	29	1563	3934	63483496
Mucosal inflammation	135.63	87.80	49	1543	46879	63440551
Cytomegalovirus infection	121.37	87.80	37	1555	20915	63466515
Acute graft versus host disease	110.73	87.80	25	1567	4403	63483027
Skin toxicity	109.17	87.80	25	1567	4689	63482741
Graft versus host disease in gastrointestinal tract	101.46	87.80	22	1570	3219	63484211
Adenovirus reactivation	101.08	87.80	14	1578	137	63487293
Varicella zoster virus infection	99.77	87.80	21	1571	2668	63484762

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
Cytomegalovirus infection	308.65	61.20	99	2142	26036	34928654
Graft versus host disease in skin	178.73	61.20	43	2198	3882	34950808
Mucosal inflammation	167.44	61.20	70	2171	38552	34916138
Cytomegalovirus infection reactivation	167.39	61.20	43	2198	5075	34949615
Adenovirus infection	161.39	61.20	42	2199	5215	34949475
Graft versus host disease in gastrointestinal tract	150.55	61.20	37	2204	3646	34951044
Acute graft versus host disease in skin	128.48	61.20	35	2206	5166	34949524
Off label use	107.43	61.20	132	2109	419392	34535298
Human herpesvirus 6 infection	90.56	61.20	22	2219	2059	34952631
Pneumatosis intestinalis	85.78	61.20	24	2217	3899	34950791
Acute graft versus host disease in intestine	84.81	61.20	22	2219	2686	34952004
Cytomegalovirus viraemia	82.65	61.20	27	2214	7403	34947287
Acute graft versus host disease	77.90	61.20	25	2216	6478	34948212
Adenovirus reactivation	75.44	61.20	13	2228	213	34954477
Product use in unapproved indication	70.57	61.20	59	2182	117440	34837250
Epstein-Barr virus infection	66.17	61.20	23	2218	7605	34947085
Posterior reversible encephalopathy syndrome	63.82	61.20	24	2217	9930	34944760

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
Adenovirus infection	443.14	66.80	98	3665	8349	79732276
Cytomegalovirus infection	424.51	66.80	132	3631	42512	79698113
Graft versus host disease in skin	326.88	66.80	72	3691	6001	79734624
Cytomegalovirus infection reactivation	295.81	66.80	71	3692	8645	79731980
Acute graft versus host disease in skin	294.38	66.80	69	3694	7589	79733036
Mucosal inflammation	272.27	66.80	110	3653	75470	79665155
Human herpesvirus 6 infection	246.96	66.80	56	3707	5314	79735311
Off label use	195.70	66.80	225	3538	906990	78833635
Graft versus host disease in gastrointestinal tract	191.15	66.80	47	3716	6309	79734316
Cytomegalovirus viraemia	189.53	66.80	54	3709	12767	79727858
Adenovirus reactivation	177.36	66.80	28	3735	361	79740264
Acute graft versus host disease	155.55	66.80	44	3719	10123	79730502
Product use in unapproved indication	137.37	66.80	105	3658	250254	79490371
Acute graft versus host disease in intestine	132.26	66.80	32	3731	4009	79736616
Skin toxicity	122.74	66.80	35	3728	8279	79732346
Autoimmune haemolytic anaemia	109.12	66.80	32	3731	8348	79732277
Epstein-Barr virus infection	103.76	66.80	35	3728	14381	79726244
BK virus infection	103.22	66.80	31	3732	8773	79731852
Cytomegalovirus chorioretinitis	94.18	66.80	26	3737	5464	79735161
Epstein-Barr virus infection reactivation	72.36	66.80	17	3746	1875	79738750
Posterior reversible encephalopathy syndrome	70.14	66.80	31	3732	26250	79714375
Pneumatosis intestinalis	68.45	66.80	21	3742	6376	79734249

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01AB02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ALKYLATING AGENTS Alkyl sulfonates
MeSH PA	D000477	Alkylating Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018906	Antineoplastic Agents, Alkylating
MeSH PA	D009676	Noxae

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

Disease	Relation	SNOMED_ID	DOID
Allogeneic peripheral blood stem cell transplant	indication	425843001

🐶 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:

None

External reference:

ID	Source
D07253	KEGG_DRUG
C0076959	UMLSCUI
CHEBI:82557	CHEBI
CHEMBL455186	ChEMBL_ID
DB11678	DRUGBANK_ID
C018404	MESH_SUPPLEMENTAL_RECORD_UI
9882105	PUBCHEM_CID
8281	IUPHAR_LIGAND_ID
3103	INN_ID
CO61ER3EPI	UNII
38508	RXNORM
004465	NDDF
326774002	SNOMEDCT_US
395912000	SNOMEDCT_US

Pharmaceutical products:

None