Alkylating agents

What are Alkylating agents?

Alkylating agents are compounds that work by adding an alkyl group to the guanine base of the DNA molecule, preventing the strands of the double helix from linking as they should. This causes breakage of the DNA strands, affecting the ability of the cancer cell to multiply. Eventually, the cancer cell dies. Alkylating agents were one of the first classes of drugs to be used against cancer. There are five traditional categories of alkylating agents:

  • Nitrogen mustards (eg, bendamustine, chlorambucil, cyclophosphamide, ifosfamide, mechlorethamine, melphalan)
  • Nitrosoureas (eg, carmustine, lomustine, streptozocin)
  • Alkyl sulfonates (eg, busulfan)
  • Triazines (eg, dacarbazine, temozolomide)
  • Ethylenimines (eg, altretamine, thiotepa)

Trabectedin is classed as a tetrahydroisoquinoline alkaloid, and unlike traditional alkylating agents, it binds to the minor groove of DNA and alkylates guanine at the N2 position. Alkylating agents are effective during every phase of the life cycle of a cancer cell, which means they are effective for treating a wide range of cancers. They are most effective for treating slow-growing cancers such as leukemia and solid tumors, but are also used in the treatment of breast, lung, ovarian, and prostate cancers; lymphomas, myelomas, and sarcomas; and Hodgkin's disease. Because alkylating agents affect all cells that are dividing frequently, they are also toxic to normal cells, particularly those of the gastrointestinal tract, bone marrow, testicles, and ovaries. Note: Although the platinum-containing anticancer agents, carboplatin, cisplatin, and oxaliplatin are frequently classified as alkylating agents, they are not. They cause covalent DNA adducts by another means.

List drug with Alkylating agents

Drug Name
Alkeran
Generic name: Melphalan
Alkeran IV
Generic name: Melphalan
Cyclophosphamide
Generic name: Cyclophosphamide
Cyclophosphamide oral and injection
Generic name: Cyclophosphamide (oral/injection)
Cytoxan
Generic name: Cyclophosphamide
Cytoxan Lyophilized
Generic name: Cyclophosphamide
Mustargen
Generic name: Mechlorethamine
Belrapzo
Generic name: Bendamustine
Bendamustine
Generic name: Bendamustine
Bendeka
Generic name: Bendamustine
Bicnu
Generic name: Carmustine
BiCNU injection/implant
Generic name: Carmustine (injection/implant)
Busulfan
Generic name: Busulfan
Busulfan oral/injection
Generic name: Busulfan (oral/injection)
Busulfex
Generic name: Busulfan
Carboplatin
Generic name: Carboplatin
Carmustine (Implantation)
Generic name: Carmustine
Carmustine (Intravenous)
Generic name: Carmustine
Carmustine injection/implant
Generic name: Carmustine (injection/implant)
Ceenu
Generic name: Lomustine
Chlorambucil
Generic name: Chlorambucil
Cisplatin
Generic name: Cisplatin
Dacarbazine
Generic name: Dacarbazine
Dtic-Dome
Generic name: Dacarbazine
Eloxatin
Generic name: Oxaliplatin
Evomela
Generic name: Melphalan
Gleostine
Generic name: Lomustine
Gliadel
Generic name: Carmustine
Gliadel injection/implant
Generic name: Carmustine (injection/implant)
Hepzato
Generic name: Melphalan
Ifex
Generic name: Ifosfamide
Ifosfamide
Generic name: Ifosfamide
Leukeran
Generic name: Chlorambucil
Lomustine
Generic name: Lomustine
Lurbinectedin
Generic name: Lurbinectedin
Mechlorethamine (Intravenous)
Generic name: Mechlorethamine
Melphalan (Intra-arterial, Intravenous)
Generic name: Melphalan
Melphalan (Oral)
Generic name: Melphalan
Melphalan flufenamide
Generic name: Melphalan Flufenamide
Melphalan oral/injection
Generic name: Melphalan (oral/injection)
Oxaliplatin
Generic name: Oxaliplatin
Paraplatin
Generic name: Carboplatin
Paraplatin NovaPlus
Generic name: Carboplatin
Pepaxto
Generic name:  melphalan Flufenamide
Platinol
Generic name: Cisplatin
Platinol-AQ
Generic name: Cisplatin
Streptozocin
Generic name: Streptozocin
Temodar
Generic name: Temozolomide
Temodar (Temozolomide Intravenous)
Generic name: Temozolomide
Temodar (Temozolomide Oral)
Generic name: Temozolomide
Temozolomide (Intravenous)
Generic name: Temozolomide
Temozolomide (Oral)
Generic name: Temozolomide
Temozolomide oral/injection
Generic name: Temozolomide (oral/injection)
Tepadina
Generic name: Thiotepa
Thioplex
Generic name: Thiotepa
Thiotepa
Generic name: Thiotepa
Trabectedin
Generic name: Trabectedin
Treanda
Generic name: Bendamustine
Vivimusta
Generic name: Bendamustine
Yondelis
Generic name: Trabectedin
Zanosar
Generic name: Streptozocin
Zepzelca
Generic name:  lurbinectedin (for Injection)

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