Registration Dossier

Diss Factsheets

Administrative data

Endpoint:
basic toxicokinetics, other
Type of information:
other: Evaluation based on physicochemical and in vivo data
Adequacy of study:
key study
Study period:
21 Dec 2016
Reliability:
1 (reliable without restriction)
Rationale for reliability incl. deficiencies:
test procedure in accordance with generally accepted scientific standards and described in sufficient detail

Data source

Reference
Reference Type:
study report
Title:
Unnamed
Year:
2016
Report date:
2016

Materials and methods

Objective of study:
toxicokinetics
Test guideline
Qualifier:
according to guideline
Guideline:
other: Expert Statement
Principles of method if other than guideline:
Toxicokinetic behaviour was evaluated based on physicochemical and in vivo data.
GLP compliance:
no

Test material

Constituent 1
Chemical structure
Reference substance name:
Sodium 1-amino-4-[[3,5-bis[[(chloroacetyl)amino]methyl]-2,4,6-trimethylphenyl]amino]-9,10-dihydro-9,10-dioxoanthracene-2-sulphonate
EC Number:
279-365-5
EC Name:
Sodium 1-amino-4-[[3,5-bis[[(chloroacetyl)amino]methyl]-2,4,6-trimethylphenyl]amino]-9,10-dihydro-9,10-dioxoanthracene-2-sulphonate
Cas Number:
80010-51-1
Molecular formula:
C29H28Cl2N4O7S.Na
IUPAC Name:
sodium 1-amino-4-[(3,5-bis{[(chloroacetyl)amino]methyl}-2,4,6-trimethylphenyl)amino]-9,10-dioxo-9,10-dihydroanthracene-2-sulfonate
Test material form:
solid: particulate/powder
Remarks:
migrated information: powder
Details on test material:
Identification: FAT 21036/G TE
Lot: AT-0033945200
Appearance: Dark blue powder
Specific details on test material used for the study:
Substance name: FAT 21036/G TE
Batch/Lot number: AT-0033945200
Appearance: Blue solid
Purity: 64.5 %
Molecular weight: 669.52 g/mol
Specific gravity: 1.6400 mg/mL

Results and discussion

Preliminary studies:
From the information provided it has been concluded that the absorption of FAT 21036/G would primarily take place in the gastrointestinal tract following oral ingestion with some absorption potentially also capable of taking place via damaged skin albeit uptake via intact skin is considered unlikely to occur. FAT 21036/G once absorbed would in all probability be distributed in serum with excretion via the urine and faeces.

Metabolite characterisation studies

Metabolites identified:
not measured

Applicant's summary and conclusion

Conclusions:
From the information provided it has been concluded that the absorption of FAT 21036/G would primarily take place in the gastrointestinal tract following oral ingestion with some absorption potentially also capable of taking place via damaged skin albeit uptake via intact skin is considered unlikely to occur. FAT 21036/G once absorbed would in all probability be distributed in serum with excretion via the urine and faeces.
Executive summary:

The absorption, distribution, metabolism and excretion of FAT 21036/G has been predicted based on the physico-chemical properties and supporting toxicological information provided for FAT 21036/G.

FAT 21036/G is indicated to be highly water soluble and would most likely following oral administration be absorbed in the gastro-intestinal tract with subsequent systemic distribution taking place via the serum.

The physico-chemical properties indicate the risk of inhalation to be minimal and in the event any did take place the available supporting toxicological information indicates no elevated toxicity would be anticipated. There was no confirmatory evidence to indicate how FAT 21036/G or any of its intermediate products are metabolised however the hydrophilic nature of FAT 21036/G would suggest passage across biological membranes would be limited.

Furthermore, the histopathological evidence derived from a repeated dose toxicity study with an analogue of FAT 21036/G provided no conclusive evidence of test item or metabolite influenced hepatic metabolism. Neither was there evidence to confirm the route of excretion; nevertheless, it is reasonable to assume that due to FAT 21036/G being highly water soluble clearance would likely be via the urine with any remaining test item not absorbed being excreted in the faeces. Based on review of the available information it has therefore been concluded the risk of systemic toxicity from FAT 21036/G would be minimal.