クロラムブシル
Chlorambucil
4-[bis(2-chloroethyl)amino]benzenebutanoic acid
別名: Leukeran · Chloraminophene · Linfolysin · CB-1348 · NSC-3088 · WR-139013 · chlorambucilum · chlorbutinum
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
0.1-0.2 mg/kg PO once daily or every other dayPO· q24h or q48h
— 🐕
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Adjunctive therapy for glomerulonephritis | 0.1-0.2 mg/kg PO once daily or every other day | PO | q24h or q48h | — | 🌎 NA |
| Canine lymphoma (first level treatment when combination chemo is declined) | 6-8 mg/m2 (NOT mg/kg) PO every other day | PO | q48h | — | 🌎 NA |
| Lymphoproliferative disease; macroglobulinemia | 2-4 mg/m2 (NOT mg/kg) PO q24-48h | PO | q24-48h | — | 🌎 NA |
| Pemphigus complex | 0.2 mg/kg q24-48h | PO | q24-48h | — | 🌎 NA |
| Pemphigus complex | 0.1-0.2 mg/kg once daily initially until marked improvement (or 75% improvement) of clinical signs (may require 4-8 weeks). Then alternate day dosing is begun and maintained for several weeks. | PO | q24h initially, then q48h | Several weeks | 🌎 NA |
| Adjunctive treatment of inflammatory bowel disease | 1.5 mg/m2 (NOT mg/kg) PO every other day | PO | q48h | — | 🌎 NA |
| Chronic lymphocytic leukaemia | 2-6 mg/m2 initially until remission achieved, then at reduced dosage/frequency; OR 0.2 mg/kg for 7 days then 0.1 mg/kg for maintenance; OR 20 mg/m2 every 1-2 weeks | PO | q24h or q1-2wk | Until remission, then maintenance | 🌍 EU |
| Lymphoma | 15-20 mg/m2 with prednisolone; OR 2-6 mg/m2; OR 1.4 mg/kg as single dose substitute for cyclophosphamide in CHOP-type protocols | PO | q2wk (15-20 mg/m2) or q24-48h (2-6 mg/m2) | Protocol dependent | 🌍 EU |
| Pemphigus complex | 0.1-0.2 mg/kg initially until marked improvement, then alternate-day dosing | PO | q24h initially, then q48h | Often for several weeks | 🌍 EU |
| Protein-losing enteropathy and other immune-mediated diseases | 2-6 mg/m2 until clinical remission, then tapered to the minimum effective dose | PO | q24h | Until remission, then tapered | 🌍 EU |
| Metronomic chemotherapy | 4 mg/m2 | PO | q24h | Ongoing | 🌍 EU |
- Canine lymphoma (first level treatment when combination chemo is declined): Used in combination with Prednisone 40 mg/m2 PO daily for 7 days then every other day. Perform CBC every 2-3 weeks.
- Pemphigus complex: With Prednisone 2-4 mg/kg PO divided q12h
- Pemphigus complex: Used in combination with corticosteroids. Alternately decrease chlorambucil and corticosteroids until lowest possible dose is attained.
- Chronic lymphocytic leukaemia: Give with food. Often used with prednisolone 40 mg/m2 p.o. q24h for 7 days then 20 mg/m2 q48h.
- Lymphoma: Give with food.
- Pemphigus complex: Give with food. Used in combination with corticosteroids.
- Protein-losing enteropathy and other immune-mediated diseases: Give with food.
- Metronomic chemotherapy: Give with food.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Refractory or severe IBD (Cats > 4 kg) | 2 mg (total dose) PO q48 hours (every other day) for 2-4 weeks then tapered to the lowest effective dose (2 mg per cat q72-96 hours; every 3rd to 4th day) | PO | q48h initially, then q72-96h | Indefinite | 🌎 NA |
| Refractory or severe IBD (Cats < 4 kg) | 2 mg (total dose) q72 hours (every 3rd day) | PO | q72h | — | 🌎 NA |
| Severe IBD or intestinal lymphoma | 15 mg/m2 (NOT mg/kg) PO once per day for 4 consecutive days, repeated every 3 weeks | PO | q24h for 4 days, repeat q3w | — | 🌎 NA |
| Lymphocytic-plasmacytic enteritis (LPE) - Method 1 | Initial dose is 2 mg/m2 (NOT mg/kg) PO for 4-7 days, then decreased to 1 mg/m2 (NOT mg/kg) for 7 days. If clinical signs are lessening, continue daily dosing but only every other week | PO | Variable | — | 🌎 NA |
| Lymphocytic-plasmacytic enteritis (LPE) - Method 2 | Large cats (>7 lb.) 2 mg PO twice weekly; smaller cats (<7 lb) 1 mg PO twice weekly | PO | Twice weekly | — | 🌎 NA |
| Severe IBD / Lymphoma (Alternative to prednisolone) | For cats < 2 kg: 2 mg (total dose) PO once weekly. For cats > 2 kg: 2 mg (total dose) PO once every 4 days. | PO | Once weekly or q4d | — | 🌎 NA |
| Pemphigus complex or other immune-mediated dermatoses | 2 mg (total dose per cat) every 48 hours | PO | q48h | — | 🌎 NA |
| Generalized pemphigus foliaceous | 0.1-0.2 mg/kg PO q24-48h | PO | q24-48h | — | 🌎 NA |
| Idiopathic dermatitis | 0.2 mg/kg PO q24-48h | PO | q24-48h | — | 🌎 NA |
| Adjunctive treatment of FIP | 20 mg/m2 (NOT mg/kg) every 2-3 weeks | PO | q2-3w | — | 🌎 NA |
| Lymphocytic leukemia | 6 mg/m2 (2 mg/5.3 kg cat) PO every other day | PO | q48h | — | 🌎 NA |
| Immune-mediated disease | >4 kg: 2 mg (total dose); <4 kg: 2 mg (total dose) | PO | q48h (>4 kg) or q72h (<4 kg) | 2-4 weeks, then tapered to lowest effective dose | 🌍 EU |
| Chronic lymphocytic leukaemia | 2 mg/m2 OR 20 mg/m2 | PO | q48h (2 mg/m2) or q14d (20 mg/m2) | Ongoing | 🌍 EU |
| Low grade/small cell lymphoma | 20 mg/m2 | PO | q14d | Ongoing | 🌍 EU |
| Substitute for cyclophosphamide in CHOP protocol | 1.4 mg/kg | PO | Once | Single dose | 🌍 EU |
| Feline pemphigus foliaceus or severe feline eosinophilic granuloma complex | 0.1-0.2 mg/kg initially until marked improvement, then alternate-day dosing | PO | q24h initially, then q48h | Often for several weeks | 🌍 EU |
- Refractory or severe IBD (Cats > 4 kg): Second choice after corticosteroids
- Severe IBD or intestinal lymphoma: In combination with prednisolone. Alternatively, may dose at 2 mg (total dose) per cat every 4 days indefinitely.
- Lymphocytic-plasmacytic enteritis (LPE) - Method 1: Administer with prednisolone. Common for patients to develop anemia.
- Lymphocytic-plasmacytic enteritis (LPE) - Method 2: Slowly taper to lowest effective dose after 4-6 weeks.
- Pemphigus complex or other immune-mediated dermatoses: May be used in combination with or as an alternative to steroids.
- Generalized pemphigus foliaceous: Add if poor response to prednisolone alone.
- Idiopathic dermatitis: Closely monitor during treatment.
- Adjunctive treatment of FIP: With Prednisolone 4 mg/kg PO once daily
- Lymphocytic leukemia: With prednisolone 5 mg/cat/day. Supplemental cobalamin and folate/B-complex vitamins should also be given.
- Immune-mediated disease: Give with food.
- Chronic lymphocytic leukaemia: Give with food. With or without prednisolone.
- Low grade/small cell lymphoma: Give with food. Used with prednisolone.
- Substitute for cyclophosphamide in CHOP protocol: Give with food.
- Feline pemphigus foliaceus or severe feline eosinophilic granuloma complex: Give with food. Used in combination with corticosteroids.
馬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Adjunctive therapy in treating lymphoma using the LAP protocol | 20 mg/m2 (NOT mg/kg) PO every 2 weeks | PO | q2w | — | 🌎 NA |
- Adjunctive therapy in treating lymphoma using the LAP protocol: Alternating with cytosine arabinoside and Prednisone 1.1-2.2 mg/kg PO every other day.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
クロラムブシルはナイトロジェンマスタード誘導体であり、獣医学において主に抗悪性腫瘍薬および免疫抑制剤として使用されます。
- 臨床のポイント: 猫の重度自己免疫疾患（炎症性腸疾患、落葉状天疱瘡など）や小細胞性（低悪性度）消化器型リンパ腫の治療において、シクロホスファミドやアザチオプリンなどの他のアルキル化剤と比較して毒性が著しく低く、忍容性が高いため、猫の医療で非常に好まれています。
- また、リンパ性白血病、多発性骨髄腫、真性多血症、マクログロブリン血症などの様々な腫瘍性疾患にも使用されます。
- 骨髄抑制を引き起こす可能性があるため、治療中は全血球計算（CBC）の定期的なモニタリングが不可欠です。
作用機序
Chlorambucil is a cell-cycle nonspecific alkylating agent.
- Mechanism: It works by forming highly reactive carbonium ions that cross-link with cellular DNA → prevents DNA transcription and replication → disrupts nucleic acid function → ultimately leads to cell death (apoptosis).
- Its immunosuppressive effects are secondary to its cytotoxic action on rapidly dividing lymphoid cells.
安全性・警告
禁忌
- Known hypersensitivity or resistance to the drug
- Pregnancy (potential teratogen)
有害事象
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Gastrointestinal toxicity (vomiting, diarrhea)
- Alopecia and delayed hair regrowth (especially in Poodles and Kerry Blue Terriers)
- Neurotoxicity (rare; facial twitching, myoclonus, agitation, seizures)
注意事項
Important Warnings:
- Myelosuppression: Use with extreme caution in patients with preexisting bone marrow depression or active infections.
- Toxicity: Higher dosages increase the likelihood of toxicity. Nadirs usually occur within 7-14 days of starting therapy.
- Reproductive Safety: Potential teratogen. Avoid during pregnancy unless benefits clearly outweigh risks. Documented to cause irreversible infertility in male humans.
- Handling: Caregivers should wear gloves when handling this medication to prevent accidental exposure.
医薬品相互作用
Chloramphenicol
Additive bone marrow depression
Flucytosine
Additive bone marrow depression
Amphotericin B
Additive bone marrow depression
Colchicine
Additive bone marrow depression
Azathioprine
Increased risk of infection and immunosuppression
Cyclophosphamide
Increased risk of infection and immunosuppression
Cyclosporine
Increased risk of infection and immunosuppression
Corticosteroids
Increased risk of infection and immunosuppression
Hepatic cytochrome P450 stimulatorsMajor
Increases cytotoxic effects of chlorambucil
PrednisoloneMinor
Synergistic effect in the management of lymphoid neoplasia
監視
- Clinical efficacy
- CBC and Platelets (once weekly or every other week initially; once stable, monthly or every 3-6 months)
- Uric acid levels (if warranted)
- Liver enzymes (if warranted)
薬物動態
吸収
Rapidly and nearly completely absorbed after oral administration; peak levels occur in about one hour.
分布
Highly bound to plasma proteins. Crosses the placenta. Unknown if it crosses the blood-brain barrier, but neurological side effects have been reported.
代謝
Extensively metabolized in the liver, primarily to phenylacetic acid mustard, which is active.
消失
Phenylacetic acid mustard is further metabolized to other metabolites that are excreted in the urine.
過剰投与
The oral LD50 in mice is 123 mg/kg. In humans, acute overdoses up to 5 mg/kg resulted in neurologic toxicity (seizures) and pancytopenia (nadirs at 1-6 weeks post ingestion).
- Treatment: Consists of gut emptying when appropriate (beware of rapidly changing neurologic status if inducing vomiting).
- Monitoring: CBCs several times a week for several weeks should be performed. Blood component therapy may be necessary.
製品
製剤
- tablets
- oral suspension (compounded)
ヒト用医薬品
- Chlorambucil Oral Tablets (film-coated): 2 mg; Leukeran® (GlaxoSmithKline); (Rx)
規制ステータス
European Union✗ 未承認処方箋医薬品EMA
POM (Prescription Only Medicine). Handled under strict cytotoxic drug regulations.
United Kingdom✗ 未承認処方箋医薬品VMD
POM. Handled under strict cytotoxic drug regulations.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Tablets should be stored in light-resistant, well-closed containers under refrigeration (2-8°C; 36-46°F). Tablets can be stored at a maximum of 30°C (86°F) up to one week. Compounded oral suspensions (2 mg/mL) retain 90% potency for 7 days at 5°C; room temperature storage causes rapid decomposition.
飼主向け情報
飼い主様への重要な情報
- 投薬: 獣医師の指示通りに正確に投薬してください。獣医師に相談せずに用量を変更したり、急に投薬を中止したりしないでください。
- 安全な取り扱い: これは抗がん剤であるため、錠剤や懸濁液を取り扱う際は手袋を着用してください。取り扱い後は手をよく洗ってください。妊娠中の女性はこの薬の取り扱いを完全に避けるべきです。
- 注意すべき症状: 毒性の兆候が見られた場合は、直ちに獣医師に報告してください。これには、異常な出血、原因不明のあざ、尿や便への血液の混入、重度の無気力、感染の兆候（発熱など）、息切れなどが含まれます。
- モニタリング: 薬が骨髄を過度に抑制していないか確認するため、ペットには定期的な血液検査が必要です。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。