Peringatan Keamanan

Side effects observed from the topical application of cantharidin include blistering, erythema, pain, bleeding, ring warts, post-inflammatory hyperpigmentation, lymphangitis, secondary bacterial cellulitis, scarring, and varicelliform vesicular dermatitis.A32892

Oral ingestion of cantharidin has resulted in renal failure, blistering and severe damage to the gastrointestinal tract, coagulopathy, seizures, and flaccid paralysis. In the event that YCANTH topical solution is ingested, patients should seek medical attention immediately and contact a Poison Center (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.L47501

Carcinogenicity studies have not been conducted with cantharidin. Cantharidin was not mutagenic in a bacteria reverse mutation (Ames) assay. An in vitro chromosomal aberration assay in human lymphocytes with cantharidin was inconclusive. Cantharidin was positive in an in vitro micronucleus assay in TK6 cells, primarily through an aneugenic mechanism. The effects of cantharidin on fertility have not been evaluated.L47501

Cantharidin

DB12328

small molecule approved investigational

Deskripsi

Cantharidin is a naturally occurring odorless, colorless fatty substance of the terpenoid class that is produced as an oral fluid in the alimentary canal of the male blister beetle.A32891, A32892 For its natural purpose, the male blister beetle secretes and presents the cantharidin to a female beetle as a copulatory gift during mating. Post-copulation, the female beetle places the cantharidin over her eggs as protection against any potential predators.A32891, A32892

Topical cantharidin products do not necessarily demonstrate any particular better effectiveness at treating topical skin conditions like warts than other commonly available vesicant and/or keratolytics although various studies have also investigated the possibility of using cantharidin as an inflammatory model or in cancer treatment.A32892 Regardless, the ongoing lack of FDA approval is likely related to certain toxic effects that were observed following oral ingestion, which include ulceration of the gastrointestinal and genitourinary tracts, along with electrolyte and renal function disturbance in humans and animals A32891.

Available synthetically since the 1950s, topical applications of cantharidin have been used predominantly as a treatment for cutaneous warts since that time. A32891, A32892 In 1962 however, marketers of cantharidin failed to produce sufficient efficacy data, resulting in the FDA revision of approval of cantharidin.A32892 Nevertheless, it gained its first FDA approval on Jul 21, 2023, under the brand name YCANTH™ by Verrica Pharmaceuticals for the treatment of molluscum contagiosum in adult and pediatric patients.L47496 The approval was based on positive results from 2 phase III trials, CAMP-1 and CAMP-2, where 46% and 52% of patients treated with cantharidin achieved complete molluscum clearance, respectively.L47496

Struktur Molekul 2D

Berat 196.202
Wujud -

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information has been ongoing in 2018.[L2647] There are however some studies regarding such data in animal models like beagle dogs.[A32901]
Volume Distribusi After oral or IP injection of (3)H-labeled cantharidin, high levels of radioactivity were distributed to and exhibited in the bile, kidney, liver, stomach, and tumor cells of ascites hepatoma-bearing mice. Such distribution suggests the agent has an affinity for liver and tumor tissues.[L2648] Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information has been ongoing in 2018.[L2647] There are however some studies regarding such data in animal models like beagle dogs.[A32901]
Klirens (Clearance) Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information has been ongoing in 2018.[L2647] There are however some studies regarding such data in animal models like beagle dogs.[A32901]

Absorpsi

Cantharidin is absorbed from the gastrointestinal tract, and, to a limited extent from the skin as well.L2648 Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information has been ongoing in 2018.L2647 There are however some studies regarding such data in animal models like beagle dogs.A32901

Metabolisme

Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information has been ongoing in 2018.L2647 There are however some studies regarding such data in animal models like beagle dogs.A32901

Rute Eliminasi

It has been observed that absorbed cantharidin is excreted by the kidney.L2648 Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information has been ongoing in 2018.L2647 There are however some studies regarding such data in animal models like beagle dogs.A32901

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Serine/threonine-protein phosphatase PP1-alpha catalytic subunit PPP1CA
Aryl hydrocarbon receptor AHR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27319954
    Al-Dawsari NA, Masterpol KS: Cantharidin in Dermatology. Skinmed. 2016 Apr 1;14(2):111-4. eCollection 2016.
  • PMID: 24945640
    Torbeck R, Pan M, DeMoll E, Levitt J: Cantharidin: a comprehensive review of the clinical literature. Dermatol Online J. 2014 Jun 15;20(6).
  • PMID: 20331621
    Li W, Xie L, Chen Z, Zhu Y, Sun Y, Miao Y, Xu Z, Han X: Cantharidin, a potent and selective PP2A inhibitor, induces an oxidative stress-independent growth inhibition of pancreatic cancer cells through G2/M cell-cycle arrest and apoptosis. Cancer Sci. 2010 May;101(5):1226-33. doi: 10.1111/j.1349-7006.2010.01523.x. Epub 2010 Feb 5.
  • PMID: 19938553
    Dang Y, Zhu C: Pharmacokinetics and bioavailability of cantharidin in beagle dogs. Zhongguo Zhong Yao Za Zhi. 2009 Aug;34(16):2088-91.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Canthacur-PS
    Liquid • - • Topical • Canada • Approved
  • Cantharidin 0.7%
    Liquid • 0.7 g/100g • Topical • US
  • Cantharidin 1% / Podophyllum Resin 5% / Salicylic Acid 30%
    Liquid • - • Topical • US
  • Cantharone Plus
    Liquid • - • Topical • Canada • Approved
  • Ycanth
    Solution • 3.20 mg/0.45mL • Topical • US • Approved
  • Ycanth
    Solution • 3.20 mg/0.45mL • Topical • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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