JP2010184936A5

JP2010184936A5 -

Info

Publication number: JP2010184936A5
Application number: JP2010125672A
Authority: JP
Filing date: 2010-06-01
Publication date: 2011-03-31

Claims

An agent for treating a human subject exposed to ionizing radiation, the agent comprising a compound of structural formula (I):

(Where, in the formula,
R ₁ is a hydrogen atom, a lower alkyl group, a sulfur-containing amino acid, or

R ₂ and R ₄ each independently represent SO ₃ ⁻ M ⁺ , PO ₃ ²⁻ M ₂ ²⁺ , or PO ₂ S ²⁻ M ₂ ^2+.
R ₃ and R ₅ are each independently a hydrogen atom, a hydroxyl group, or a sulfhydryl group. When R ₁ is a hydrogen atom, R ₃ is not a sulfhydryl group.
m and n are each independently 0, 1, 2, 3, or 4, provided that when m or n is 0, R ₃ is a hydrogen atom, and
M is a hydrogen atom or an alkali metal ion. )
Or a pharmaceutically acceptable salt thereof, and an effective amount administered parenterally or orally to the subject after the subject has been exposed to ionizing radiation.

The effective amount of the compound of the structural formula (I) is 0.1 mg / kg with respect to the body weight of the subject to 1,000 mg / kg with respect to the body weight. .

An agent for pre-treatment of a human subject undergoing exposure to ionizing radiation, the agent comprising a compound of structural formula (I):

R ₂ and R ₄ each independently represent SO ₃ ⁻ M ⁺ , PO ₃ ²⁻ M ₂ ²⁺ , or PO ₂ S ²⁻ M ₂ ^2+.
R ₃ and R ₅ are each independently a hydrogen atom, a hydroxyl group, or a sulfhydryl group. When R ₁ is a hydrogen atom, R ₃ is not a sulfhydryl group.
m and n are each independently 0, 1, 2, 3, or 4, provided that when m or n is 0, R ₃ is a hydrogen atom, and
M is a hydrogen atom or an alkali metal ion. )
Or a pharmaceutically acceptable salt thereof, wherein an effective amount is administered parenterally or orally to the subject 15 minutes to 1 hour before exposure to the ionizing radiation.

R ₂ and R ₄ each independently represent SO ₃ ⁻ M ⁺ , PO ₃ ²⁻ M ₂ ²⁺ , or PO ₂ S ²⁻ M ₂ ^2+.
R ₃ and R ₅ are each independently a hydrogen atom, a hydroxyl group, or a sulfhydryl group. When R ₁ is a hydrogen atom, R ₃ is not a sulfhydryl group.
m and n are each independently 0, 1, 2, 3, or 4, provided that when m or n is 0, R ₃ is a hydrogen atom, and
M is a hydrogen atom or an alkali metal ion. )
Or a pharmaceutically acceptable salt thereof and an effective dose administered parenterally or orally to the subject 15 minutes to 1 hour prior to exposure to the ionizing radiation. ,
Here, an effective dosage when the compound of the structural formula (I) is added is administered about 2 hours after the radiation exposure.

5. The medicament of claim 4, wherein the additional effective dosing is administered to the subject about every 4 hours after the first mentioned effective additional dosing.

The medicament according to claim 4, wherein the additional effective dosing is performed orally or intravenously.

The compound according to any one of claims 1 to 6, wherein the compound of the structural formula (I) is 2,2'-dithiobisethanesulfonic acid or a pharmaceutically acceptable salt thereof.

The compound according to any one of claims 1 to 7, wherein the compound of the structural formula (I) is 2,2'-dithiobisethanesulfonic acid or a disodium salt thereof.

The compound according to any one of claims 1 to 8, wherein the compound of the structural formula (I) is dimesna.

10. A drug according to any one of claims 1 to 9, wherein the compound of structural formula (I) is administered intravenously.

10. A drug according to any one of claims 1 to 9, wherein the compound of structural formula (I) is administered by intravenous injection.

3. The medicament according to claim 2, wherein the effective amount is 20 mg / kg to 1000 mg / kg of body weight of the subject.

12. An effective amount of a compound of structural formula (I) is 0.1 mg / kg to body weight of the subject to 1,000 mg / kg body weight, The drug according to one item.

An effective amount of the compound of structural formula (I) is 500 mg / m ^２2 ~ 40g / m ^２2 The drug according to any one of claims 3 to 11, which is

An agent for pre-treatment of a human subject who is exposed to ionizing radiation exposure, wherein the weight of the subject is changed from 0.1 mg / kg to body weight 15 minutes to 1 hour before being exposed to the ionizing radiation. 4. The drug according to claim 3, which is dimesna administered intravenously or orally in an effective amount of 1,000 mg / kg.