Valrubicin

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H301：삼키면 유독함

  H312：피부와 접촉하면 유해함

  H332：흡입하면 유해함

  H340：유전적인 결함을 일으킬 수 있음 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재)

  H351：암을 일으킬 것으로 의심됨 (노출되어도 암을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재)

  H360：태아 또는 생식능력에 손상을 일으킬 수 있음

• 예방조치문구

  P201：사용 전 취급 설명서를 확보하시오.

  P202：모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P270：이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

  P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P281：요구되는 개인 보호구를 착용하시오

  P301+P310：삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

  P308+P313：노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.

  P312：불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P321：(…) 처치를 하시오.

  P322：특정 조치(라벨의 … 참조)

  P330：입을 씻어내시오.

  P363：다시 사용전 오염된 의류는 세척하시오.

  P405：밀봉하여 저장하시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

Valrubicin 화학적 특성, 용도, 생산

• 개요

  Valrubicin was launched as a new 'chemotherapeutic agent for the treatment of bladder cancer, particularly in patients with BCG-refractory carcinoma in situ (CIS) of the bladder for whom immediate cystectomy is unacceptable. It belongs to the class of anthracyclines, the widest used in human cancers, and is a N-trifluoroacetyl 14-valerate derivative of doxorubicin.Valrubicin can be obtained in 3 steps from daunomycin by N-trifluoroacetylation of the sugar moiety then iodination of the 2-acetyl group and introduction of a valerate residue. A proposed mechanism involved in the cytotoxicity of Valrubicin coud be the blockade of SV40 large T antigen helicase; this cellular enzyme is involved in the formation of a ternary complex with DNA to maintain the topographic structure of DNA during transcription. In patients with CIS of bladder refractory to front line and second line therapies, intravesical instillation of Valrubicin resulted in a complete response with a significant rate and allowed a delay in cystectomy. Systemic absorption was minimal and accordingly produced a lower incidence of cardiotoxicity compared with doxorubicin.

• 화학적 성질

  Red Solid

• 용도

  Chemotherapy drug used to treat cancer of the bladder.

• 일반 설명

  Valrubicin is available in 200-mg vials for intravesicular administrationin the treatment of bladder cancer (orphan drugstatus). The increased lipophilicity associated with the valericacid ester and trifluoro acetate functionalities increasestissue penetration and remains intact because, in large measure,of the lack of exposure to hydrolyzing enzymes causedby direct delivery into the bladder followed by voiding ofthe instilled solution. This local action also minimizes cardiotoxicityand other adverse effects seen with other anthracyclines.The major adverse effects that are seen are bladderirritation and reddening of the urine.

• Mechanism of action

  Valrubicin is an anthracycline that affects a variety of interrelated biological functions, most of which involve nucleic acid metabolism. In cells, it inhibits the incorporation of nucleosides into nucleic acids, causes chromosomal damage, and arrests the cell cycle in G2. Although valrubicin does not bind strongly to DNA, valrubicin metabolites interfere with the normal DNA breaking-resealing action of DNA topoisomerase II.

• Clinical Use

  Valrubicin currently has orphan drug status in the treatment of bacille Calmette-Guérin (BCG)–refractory bladder cancer (the total patient population is ~1,000 individuals) and is used with patients for whom surgical intervention would result in high morbidity or death.

• 부작용

  The most commonly reported adverse reactions are abdominal pain, urinary tract infection, hematuria, and dysuria. Systemic exposure to the drug and its metabolites would, of course, be greater in patients whose bladder wall integrity has been compromised by disease, and these patients should not receive valrubicin.

• Safety Profile

  Poison by intraperitoneal route.Human mutation data reported. When heated todecomposition it emits toxic fumes of Fí and NOx.

• 신진 대사

  It is administered directly into the bladder through a catheter (intravesically). The lipophilic drug is water insoluble, but it dissolves in an aqueous vehicle that includes polyoxyethylene glycol and ethanol. The patient retains the drug in the bladder for 2 hours, then voids the solution in the normal fashion. Valrubicin is active as administered, and despite the fact that hydrolysis of the ester and trifluoroacetamide can be envisioned, it is excreted essentially unchanged. Less than 1% of an administered dose is absorbed systemically, so there is essentially no exposure to metabolizing enzymes. The reduced C13-alcoholic metabolite does not form to any appreciable extent during the 2-hour treatment period. Therapy is considered to be almost exclusively local, and there is little risk for cardiac toxicity, bone marrow suppression, drug–drug interactions, or other side effects.

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