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WO1993023066A1 - Promoteur de croissance de plaquettes - Google Patents

Promoteur de croissance de plaquettes Download PDF

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Publication number
WO1993023066A1
WO1993023066A1 PCT/JP1993/000487 JP9300487W WO9323066A1 WO 1993023066 A1 WO1993023066 A1 WO 1993023066A1 JP 9300487 W JP9300487 W JP 9300487W WO 9323066 A1 WO9323066 A1 WO 9323066A1
Authority
WO
WIPO (PCT)
Prior art keywords
platelet count
group
day
administration
blood
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP1993/000487
Other languages
English (en)
Japanese (ja)
Inventor
Masahiro Maeda
Susumu Sato
Kazuyuki Otsuka
Shingo Suzuki
Mineo Niwa
Fusako Nishigaki
Kyoichi Shimomura
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Fujisawa Pharmaceutical Co Ltd
Original Assignee
Fujisawa Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Fujisawa Pharmaceutical Co Ltd filed Critical Fujisawa Pharmaceutical Co Ltd
Publication of WO1993023066A1 publication Critical patent/WO1993023066A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides

Definitions

  • the present invention relates to a platelet number enhancer (platelet number increasing agent) containing FK 565 represented by the following formula or a pharmaceutically acceptable salt thereof as an active ingredient, and is used in the field of medicine.
  • FK565 has an immunopotentiating effect and is known to be useful as an anticancer agent, an anti-AIDS agent, an antiviral agent, etc. (Japanese Patent Application Laid-Open Nos. 56-45449, 60-104019) And JP-A-64-38030).
  • the invention is based on the formula
  • F ⁇ 565 or a pharmaceutically acceptable salt thereof is useful as a platelet count reduction inhibitor, a decreased platelet count increase agent, a prophylactic or therapeutic agent for thrombocytopenia, a prophylactic or therapeutic agent for purpura, etc. is there.
  • F ⁇ 565 or a pharmaceutically acceptable salt thereof is, for example, Since it antagonizes side effects such as thrombocytopenia due to administration of anti-cancer drugs without impairing the efficacy of anti-cancer drugs such as ittomycin C and cis-bratin, it is also useful as an anti-cancer drug side effect reducer is there.
  • Pharmaceutically acceptable salts of FK565 include, for example, organic or inorganic salts such as sodium salt, potassium salt, calcium salt, ammonium salt, ethanolamine salt, triethylamine salt, dicyclohexylamine salt, and severe acids.
  • Organic or inorganic acids such as salt, trifluorophosphate, lactate, maleate, fumarate, tartrate, citrate, methanesulfonate, hydrochloride, sulfate, ganate, phosphate, etc.
  • the FK565 of the present invention can be used in the form of a solid, semisolid or liquid preparation containing a mixture with an organic or inorganic carrier or excipient suitable for oral or parenteral administration.
  • the FK565 of the present invention is used in, for example, tablet pellets, capsules, suppositories, solutions, emulsions, suspensions, and usually mixed with non-toxic and pharmaceutically acceptable carriers to form appropriate dosage forms.
  • the carriers used here are water, glucose, lactose, gum arabic, gelatin, mannitol, starch paste, magnesium sulfate, talc, methylcellulose, polyethylene glycol, corn starch, keratin, colloidal silica, and potato starch.
  • FK565 When FK565 is applied to humans or animals, it can be administered by intravenous injection, subcutaneous injection, intramuscular injection or oral administration.
  • the dose of FK565 of the present invention varies depending on conditions such as the age of each individual patient to be treated and the degree of the disease, but generally, the daily dose of the active ingredient for humans or animals is high. 0.01-1 Omg / kg is administered for prophylaxis or treatment. The platelet count increasing activity of FK565 will be described below.
  • a single intravenous dose of FK565 (0.1 mg / kg or 0.1 mg / kg) is given to three normal cynomolgus monkeys, blood is collected daily, and the platelet count is measured by SysmexE—4000 (automatic blood cells). The number was automatically measured using a counting device (Toa Medical Electronics Co., Ltd.). As a control, blood was collected from the same individual the day before administration. Separately, a saline was administered to the control group.
  • the platelet count in each group was calculated by setting the platelet count on the day before the administration as 100% for the platelet count in each dose.
  • Table 1 shows the test results.
  • FK565 (0.01 mg / kg. O.lmgZkg or l.OmgZkg) was administered to normal mice (five ddY female mice (7 weeks old) purchased from Nippon S.L.C.) in a single intravenous dose of 25 mg / day. Blood samples were collected and the platelet count was automatically measured using Sysmex E-4000. Separately, a saline was administered to the control group.
  • the platelet count in each dose was calculated with the platelet count in the control group taken as 100%.
  • Table 2 shows the test results. Test results
  • mice (ddY female mice (7 weeks old) purchased from Japan SLC, Inc.) FK565 (0.01 mg / kg. O.lmgZkg or l.Omg / kg) once a day for 3 days, and blood is collected daily, and the platelet count is measured using Sysmex E-4000. And automatic measurement. Separately, saline was administered to the control group.
  • the platelet count in each dose was calculated with the platelet count in the control group taken as 100%.
  • FK565 O.lmgZkg or l.OmgZkg
  • normal mice five ddY female mice (7-week-old) purchased from Nippon S.L.C.
  • the platelet count was automatically measured using Sysmex E-4000.
  • mice normal mice (ddY female mice (7 weeks old) purchased from S.L.C.) FK565 (0.01 mg / kg, O.lmg / Zkg or l.Omg / kg) was administered once intravenously or orally to 5 of them, and blood was collected daily and the platelet count was measured using Sysmex E-4000. Was measured automatically. A saline was administered to the control group.
  • the change in platelet count at each dose is calculated as u.
  • MMC manufactured by Kyowa Hakko Co., Ltd.
  • 5.6 mg Zkg was intravenously administered to ddY female 'mice (7 weeks old) (5 animals per group) (this administration day is hereafter referred to as dayO.
  • the day is called day2.
  • FK565 0.1 mg / kg was intravenously administered once a day from dayO to 2 for 3 days, blood was collected on day9, and the platelet count was measured automatically using Sysmex E-4000.
  • a group to which MMC was administered but not to FK565 was used as a control.
  • the change in platelet count in each group was calculated with the platelet count in the group (saline-administered group) not receiving MMC as 100%.
  • MMC manufactured by Kyowa Hakko Co., Ltd.
  • MMC manufactured by Kyowa Hakko Co., Ltd.
  • FK565 O.lmgZkg once daily
  • the dose was intravenously administered for four days from day O to 3, and blood was collected on day 8 and day 10 and the platelet count was automatically measured using Sysmex E-4000.
  • a group to which MMC was administered but not to FK565 was used as a control.
  • the change in platelet count in each group was calculated, with the platelet count in the group not receiving MMC (saline-administered group) as 100%.
  • the platelet count gradually decreased and reached a nadir at day 10 (down to 32.6% of the saline-administered control group), and then recovered slowly.
  • the decrease in platelet count due to MMC administration was significantly suppressed at daylO.
  • Blood was collected from the brachial vein of the monkey using a 2.5 ml syringe (pre-filled with 15% EDTA4Na (pH 8.0) 20 / z1 as an anticoagulant). It was stored under ice cooling until the platelet count was measured.
  • FK565 is useful for the treatment and prevention of thrombocytopenia caused by anticancer drugs and the like.
  • Starch 50mg The above components are formulated into tablets by a conventional method.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Promoteur de croissance de plaquettes contenant du FK566, substance représentée par la formule (I), ou sel de cette substance, pharmaceutiquement acceptable en tant qu'ingrédient actif.
PCT/JP1993/000487 1992-05-08 1993-04-15 Promoteur de croissance de plaquettes Ceased WO1993023066A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP4/143174 1992-05-08
JP14317492 1992-05-08

Publications (1)

Publication Number Publication Date
WO1993023066A1 true WO1993023066A1 (fr) 1993-11-25

Family

ID=15332638

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP1993/000487 Ceased WO1993023066A1 (fr) 1992-05-08 1993-04-15 Promoteur de croissance de plaquettes

Country Status (2)

Country Link
AU (1) AU3905393A (fr)
WO (1) WO1993023066A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01131121A (ja) * 1987-08-24 1989-05-24 Pitman Moore Inc 寄生体を制御する方法
EP0488041A2 (fr) * 1990-11-26 1992-06-03 Fujisawa Pharmaceutical Co., Ltd. Une composition pharmaceutique contre l'infection de cytomégalovirus

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01131121A (ja) * 1987-08-24 1989-05-24 Pitman Moore Inc 寄生体を制御する方法
EP0488041A2 (fr) * 1990-11-26 1992-06-03 Fujisawa Pharmaceutical Co., Ltd. Une composition pharmaceutique contre l'infection de cytomégalovirus

Also Published As

Publication number Publication date
AU3905393A (en) 1993-12-13

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