The antineoplastic drugs (also called cytotoxics or sometimes cytostatics) are used in treatment of malignant disease alone or in conjunction with radiotherapy, surgery or immunosuppressants. They also find application in treatment of a number of autoimmune disorders such as rheumatoid arthritis and psoriasis, and a few are used with other immunosuppressant drugs (ciclosporin, corticosteroids) to prevent transplant rejection. These other drugs are dealt with under section on immunosuppressants, .
Of all drugs discussed in this publication, antineoplastic drugs are amongst most toxic and have a low therapeutic index. This means that quite small increases in their levels can lead to development of serious and life-threatening toxicity. A list of antineoplastic drugs that are featured in this section appears in table 1 below,(below), grouped by their primary mechanism of action. This table also includes a number of hormone antagonists that are used in treatment of cancer.
Unlike most of other interaction monographs in this publication, some of information on antineoplastic drugs is derived from animal experiments and in vitro studies, so that confirmation of their clinical relevance is still needed. The reason for including these data is that anti-neoplastic drugs as a group do not lend themselves readily to kind of clinical studies that can be undertaken with many other drugs, and there would seem to be justification in this instance for including indirect evidence of this kind. The aim is not to make definite predictions, but to warn users of interaction possibilities.
1 Antineoplastics used in treatment of cancer
Alkylating agents,and drugs that appear to have an alkylating action
Carmustine,Lomustine, Streptozocin
Carboplatin,Cisplatin, Oxaliplatin
Altretamine,Busulfan, Chlorambucil, Chlormethine (Mechlorethamine), Cyclophosphamide, Dacarbazine, Estramustine, Ifosfamide, Melphalan, Temozolomide, Thiotepa
Methotrexate,Pemetrexed, Raltitrexed
Etoposide,Teniposide
Azathioprine,Cladribine, Fludarabine, Mercaptopurine, Tioguanine
Capecitabine,Carmofur, Cytarabine, Fluorouracil, Gemcitabine, Tegafur
Vinblastine,Vincristine, Vindesine, Vinorelbine
Docetaxel,Paclitaxel
Irinotecan,Topotecan, 9-Aminocamptothecin
Aclarubicin,Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone
Bleomycin,Dactinomycin, Mitomycin, Plicamycin
Bicalutamide,Flutamide, Nilutamide
Fulvestrant,Tamoxifen, Toremifene
Aminoglutethimide,Anastrozole, Exemestane, Formestane, Letrozole
Amsacrine,Asparaginase (Colaspase, Crisantaspase, Pegaspargase), Bexarotene, Erlotinib, Hydroxycarbamide, Imatinib, Mitotane, Pentostatin, Procarbazine, Sorafenib, Thalidomide, Trastuzumab, Tretinoin
| Table 1 Antineoplastics used in the treatment of cancer | |
| Action | Drugs |
| Alkylating agents, and drugs that appear to have an alkylating action | |
| Nitrosoureas | Carmustine, Lomustine, Streptozocin |
| Platinum derivatives | Carboplatin, Cisplatin, Oxaliplatin |
| Others | Altretamine, Busulfan, Chlorambucil, Chlormethine (Mechlorethamine), Cyclophosphamide, Dacarbazine, Estramustine, Ifosfamide, Melphalan, Temozolomide, Thiotepa |
| Antimetabolites | |
| Folate antagonists | Methotrexate, Pemetrexed, Raltitrexed |
| Podophylotoxin derivatives | Etoposide, Teniposide |
| Purine analogues | Azathioprine, Cladribine, Fludarabine, Mercaptopurine, Tioguanine |
| Pyridmidine analogues | Capecitabine, Carmofur, Cytarabine, Fluorouracil, Gemcitabine, Tegafur |
| Mitotic inhibitors | |
| Vinca alkaloids | Vinblastine, Vincristine, Vindesine, Vinorelbine |
| Taxanes | Docetaxel, Paclitaxel |
| Topoisomerase inhibitors | Irinotecan, Topotecan, 9-Aminocamptothecin |
| Cytotoxic antibiotics | |
| Anthracyclines | Aclarubicin, Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone |
| Others | Bleomycin, Dactinomycin, Mitomycin, Plicamycin |
| Anti-androgens | Bicalutamide, Flutamide, Nilutamide |
| Anti-oestrogens | |
| Oestrogen-receptor antagonists | Fulvestrant, Tamoxifen, Toremifene |
| Aromatase inhibitors | Aminoglutethimide, Anastrozole, Exemestane, Formestane, Letrozole |
| Miscellaneous | Amsacrine, Asparaginase (Colaspase, Crisantaspase, Pegaspargase), Bexarotene, Erlotinib, Hydroxycarbamide, Imatinib, Mitotane, Pentostatin, Procarbazine, Sorafenib, Thalidomide, Trastuzumab, Tretinoin |