Drugs and Medicinal Substances

Calicheamicin

Antineoplastic and Immunomodulating Agents

Calicheamicin is a class of enediyne antitumor antibiotics with potent cytotoxic activity against cancer cells. The molecule binds in the minor groove of DNA and undergoes a Bergman type cyclization that generates a reactive diradical species, which pulls hydrogen atoms from the sugar backbone of DNA and breaks both strands. Scientists at Lederle Laboratories isolated it from the bacterium Micromonospora echinospora in the mid 1980s, found in caliche soil deposits near Kerrville, Texas. Because it is too toxic to give on its own, it is instead attached to a targeting antibody as an antibody drug conjugate; inotuzumab ozogamicin, sold as Besponsa, carries a calicheamicin derivative to CD22 positive cells and gained United States approval in August 2017 for relapsed or refractory B cell precursor acute lymphoblastic leukemia.

Facts
Drug Class
Enediyne antitumor antibiotics 3
Mechanism of Action
Binds to the minor groove of DNA and initiates double stranded DNA cleavage via a radical abstraction process 3
First Approved / Isolated Year
1987 4
Classification
ATC ClassSourced to the subject's own account
L: Antineoplastic and Immunomodulating Agents 1
Route of Administration
Intravenous 2
Connections

Long-Form Articles

Sources
1. Anatomical Therapeutic Chemical Classification System (Wikipedia)
WikipediaFirst-level anatomical group codes, Code L
Quote, First-level anatomical group codes, Code L
Antineoplastic and immunomodulating agents
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2. Calicheamicin (Wikipedia)
Route of administrationView the Source
3. Calicheamicins (DrugFuture Chemical Data)
  • Entry description, first sentence
    Family of 15-20 enediyne antitumor antibiotics produced by Micromonospora echinospora ssp. calichensis.
  • Entry description, mechanism sentence
    Binds to the minor groove of DNA and initiates double stranded DNA cleavage via a radical abstraction process.
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4. ADC Review: Calicheamicin
Discovery history
Quote, Discovery history
Calicheamicin was isolated from Micromonospora echinospora in the mid-1980s; Lee and co-workers disclosed the discovery and structure of the calicheamicins in 1987
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