17β-hydroxy-1α-methyl-5-αandrostan-3-one acetate

Endpoint summary

Description of key information

There is no acute toxicity studies  with ZK 5894; read-across to results of studies with mesterolone (ZK 9226):
Oral (Mouse-NMRI, non-GLP): LD50 > 4000 mg/kg
[Schering AG, report dated 1968-01-10]
Subcutaneous (Mouse-NMRI, non-GLP): LD50 > 4000 mg/kg
[Schering AG, report dated 1968-01-10]
Intraperitoneal (Mouse-NMRI, non-GLP): LD50 > 4000 mg/kg
[Schering AG, report dated 1968-01-10]
Oral (Rat-Wistar, non-GLP): LD50 > 5000 mg/kg (aqueous suspension)
[Schering AG, report dated 1966-03-02]
Oral (Rat-Wistar, non-GLP): LD50 > 5000 mg/kg (oily solution)
[Schering AG, report dated 1968-05-16]
Oral (Dog-Beagle, non-GLP): LD50 > 1000 mg/kg
[Schering AG, Report No. 1498; 1974-10-28]
Intravenous (Monkey-Cynomolgus, non-GLP): LD50 > 1 mg/kg
[Schering AG, Report No. 6154; 1984-07-24]

Additional information

There is no acute toxicity studies with ZK 5894 (mesterolone acetate). Results of studies conducted with mesterolone (ZK 9226) are regarded as representative as most likely ester-cleavage occurs in vivo after administration.

The single oral administration of an aqueous microcristalline suspension of ZK 9226 to male and female mice was tolerated without any compound-related clinical or macroscopic pathological findings. The acute oral toxicity of ZK 9226 in mice is above 4000 mg/kg body weight. [Schering AG, report dated 1968-01-10]

The single subcutaneous administration of an aqueous suspension of ZK 9226 to male and female mice was tolerated without any compound-related clinical or macroscopic pathological findings. The acute subcutaneous toxicity of ZK 9226 in mice is above 4000 mg/kg body weight. [Schering AG, report dated 1968-01-10]

After single intraperitoneal administration of an aqueous suspension of ZK 9226 to male and female mice 2/5 females died on Days 1 and 2 at the dose of 4000 mg/kg. All males (5) survived the observation period. Associated clinical signs were apathy immediatetly after treatment up to Day 2. Macroscopic findings were described in individual animals at necropsy. The LD50 after intraperitoneal administration of ZK 9226 in mice is above 4000 mg/kg body weight. [Schering AG, report dated 1968-01-10]

The single oral administration of an aqueous microcristalline suspension of ZK 9226 to male and female rats was tolerated without any compound-related clinical or macroscopic pathological findings. The acute oral toxicity of ZK 9226 in mice is above 4000 mg/kg body weight. [Schering AG, report dated 1966-03-02]

The single oral administration of an oily solution of ZK 9226 to male and female rats led to mortality in 1/5 females on Day 8 at 5000 mg/kg, whereas all males (5) survived the observation period. Clinical findings in the moribund animal were cachexia and signs of local intolerance reactions in the gastrointestinal tract. The LD50 after oral administration of an oily solution of ZK 9226 to rats is above 5000 mg/kg body weight. [Schering AG, report dated 1968-05-16]

The single oral administration of ZK 9226 to male and female Beagle dogs was tolerated without any compound-related clinical findings. Acute oral toxicity of ZK 9226 is Beagle dogs is above 1000 mg/kg body weight. [Schering AG, Report No. 1498; 1974-10-28]

The single intravenous administration of ZK 9226 to male and female Cynomolgus monkeys was tolerated without any compound-related clinical findings. Acute intravenous toxicity of ZK 9226 in Cynomolgus monkeys is above 1 mg/kg body weight. [Schering AG, Report No. 6154; 1984-07-24]

Justification for classification or non-classification

Since LD50 > 2000 mg/kg after oral administration there is no classification required according to Directive 67/548/EEC and Regulation (EC) 1272/2008 (CLP).