Cyclophosphane is an antineoplastic that is converted in the body to
active alkylating metabolites with properties similar to those of chlormethine.
It also possesses marked immunosuppressant properties.
Cyclophosphane (nyclophosphamide) is widely used, often with other agents, in the treatment of malignant
diseases as indicated by the cross-references below. It is given for Burkitt's
and other non-Hodgkin's lymphomas, multiple myeloma, and mycosis fungoides. It
is also used in gestational trophoblastic tumours and malignancies of the
brain, breast, endometrium, lung, and ovary; in childhood malignancies such as
neuroblastoma, retinoblastoma, Wilms' tumour; and in sarcomas and some
The immunosuppressant properties of Nyclophosphane have been used in organ and
tissue transplantation. It has also been used in the management of disorders
thought to have an auto-immune component including amyloidosis, Behçet's
syndrome, glomerular kidney disease, idiopathic thrombocytopenic purpura,
aplastic anaemia, cryptogenic fibrosing alveolitis, polymyositis, scleroderma,
SLE, and vasculitic syndromes including the Churg-Strauss syndrome,
polyarteritis nodosa, and Wegener's granulomatosis, as indicated by the cross
Cyclophosphane is one of the most widely used drugs for the
chemotherapy of malignancy, and mention of its role may be found in the
discussions of the management of gestational trophoblastic tumours.
Cyclophosphane is also used in the management of acute lymphoblastic leukaemia
and chronic lymphocytic leukaemia.
How supplied : Sterile powder for solution for injection 0,2 g in vials.
Cytarabine is an
antimetabolic agent, a pyrimidine nucleoside analogue. Its mode of action is
due to its rapid conversion into cytosine arabinoside triphosphate, which
damages DNA when the cell cycle holds in the S phase (synthesis of DNA).
Rapidly dividing cells, which require DNA replication for mitosis, are
therefore most affected. Cytosine arabinoside also inhibits both DNA and RNA
polymerases and nucleotide reductase enzymes needed for DNA synthesis.
Cytarabine is rapidly deaminated in the body into the inactive uracil
derivative and therefore is often given by continuous intravenous infusion.
one of the mainstays of the treatment of acute myeloid leukaemias, together
with an anthracycline, and is used for the prophylaxis of meningeal leukaemia,
as well as in regimens for consolidation, in patients with acute lymphoblastic
leukaemia. It has also been investigated in the blast crisis of chronic myeloid
leukaemia and the myelodysplasias . It may be used in salvage regimens for
Hodgkin's disease, as part of the complex regimens sometimes employed in
aggressive intermediate- and high-grade non-Hodgkin's lymphomas, and for
possesses antiviral activity, and it has been used for the treatment of
generalised herpesvirus infection.
How supplied: Lyophilized powder for solution for injection 0.5 and 0.1 g in vials.
an anthracycline antineoplastic antibiotic which may act by forming a stable
complex with DNA and interfering with the synthesis of nucleic acids. It is a
cell-cycle non-specific agent. It also has actions on cell membranes, and
antibacterial and immunosuppressant properties. It is an effective
antineoplastic against a wide range of tumours as indicated by the
cross-references given below.
used, often with other antineoplastics, in the treatment of Hodgkin's disease,
non-Hodgkin's lymphomas, acute leukaemias, bone and soft-tissue sarcomas,
neuroblastoma, Wilms' tumour, and malignant neoplasms of the bladder, breast,
lung, ovary, and thyroid. It has also been used in other tumors. Liposomal
doxorubicin is used in the management of Kaposi's sarcoma in patients with AIDS
and metastatic breast and ovarian cancers.
plays a major role in combination regimens for chemotherapy of solid
malignancies; it is often employed for tumors of the breast and lung and for
Wilms tumor and neuroblastoma or retinoblastoma in children and has been used
for malignancies of the bladder; for various gynaecological cancers including
those of the endometrium, and ovary; for cancer of the liver, stomach, and
pancreas; and for neoplasms of prostate, and thymus.
doxorubicin is a component of the ABVD regimen used to treat Hodgkin's disease
and is part of the CHOP regimen used for non-Hodgkin's lymphoma. Doxorubicin is
also used in Burkitt's lymphoma, mycosis fungoides, and the lymphomas
associated with AIDS. It has been employed in acute lymphoblastic leukaemia, in
chronic lymphocytic leukaemia as part of the CHOP regimen, and in multiple
How supplied: Lyophilized powder for solution for intravenous injection 10 mg
INN: Fludarabine Phosphate
phosphate is a fluorinated nucleotide analogue of the antiviral vidarabine; it
acts as a purine antagonist antimetabolite. Fludarabine phosphate inhibits DNA
synthesis by interfering with ribonucleotide reductase and DNA polymerase. It
is active against both dividing and resting cells.
It is used for
its antineoplastic properties in the treatment of B-cell chronic lymphocytic
leukemia (CLL) and in conditioning regimes for hematopoietic cell
transplantations. Its activity in Hodgkin's disease, mycosis fungoides, and
macroglobulinemia, although suggestive, needs to be further defined and
clinical trials are warranted in hairy cell leukemia, prolymphocytic leukemia,
and previously untreated myeloma. The compound does not appear active against
most common solid tumors.
phosphate is used in various combinations with cyclophosphamide, mitoxantrone,
dexamethasone and rituximab in the treatment of indolent non-Hodgkins
lymphomas. As part of the FLAG regimen, fludarabine is used together with
cytarabine and granulocyte colony-stimulating factor in the treatment of acute
myeloid leukaemia. Because of its immunosuppressive effects, fludarabine is
also used in some conditioning regimens prior to non myeloablative allogeneic
stem cell transplant.
supplied: Lyophilized powder for solution for
injection 0.05 g in vials.
One mechanism of
action of hydroxycarbamide is believed to be based on its reduction of
production of deoxyribonucleotides via inhibition of the enzyme ribonucleotide
reductase by scavenging tyrosyl free radicals as they are involved in the
reduction NDPs. The precise mechanism of action is not yet clear, but it
appears that hydroxycarbamide increases nitric oxide levels, causing soluble
guanylyl cyclase activation with a resultant rise in cyclic GMP, and the
activation of gamma-globin synthesis necessary for fetal hemoglobin. It is
is used in the treatment of chronic myeloid leukaemia, and may be used in the
myeloproliferative disorders polycythaemia vera and primary not responding to
venipuncture and essential thrombocytosis. It has also been tried, often
combined with radiotherapy, in some solid malignancies. Hydroxycarbamide has
also produced benefit in the haemoglobinopathies, particularly in sickle-cell
disease (breaks down cells that are prone to sickle, as well as increasing
fetal hemoglobin content).
is used for the following indications: AIDS as an adjunct to ddI in combination
antiretroviral therapies, Second line treatment for psoriasis (slows down the
rapid division of skin cells).
capsules 0,25 g.
belongs to a group of drugs called antimetabolites. Leucladine produces its
anti-cancer effects by inhibiting the ability of a cell to produce DNA or
repair DNA. By inhibiting the production and repair of DNA, Leucladine
suppresses the ability of a cell to replicate or repair itself, ultimately
causing cellular death.
It is used as an
antimetabolite antineoplastic for the treatment of lymphoid malignancies
including symptomatic hairy-cell leukaemia (HCL) and chronic lymphocytic
leukaemia that does not respond to other chemotherapy agents referred to as
alkylating agents. . It is important for patients to remember that physicians
have the ability to prescribe medication for conditions other than those for
which the drug has been approved by the FDA. It has been tried in indolent
low-grade non-Hodgkin's lymphomas, histiocytic syndromes, and in
Leucladine has shown some evidence of benefit in multiple sclerosis but it is
not clear whether it improves attack rate or disease progression.
It is under
investigation for other B cell leukemias and lymphomas, such as mantle cell
lymphoma, and for multiple sclerosis.
supplied: Solution for injection 0.1% in vials.
Mercaptopurine is an antineoplastic that acts as an
antimetabolite. It is an analogue of the natural purines hypoxanthine and
adenine. After the intracellular conversion of Mercaptopurine to active nucleotides,
including thioinosinic acid, it appears to exhibit a variety of actions
including interfering with nucleic acid synthesis. It also has
immunosuppressant properties. Its actions are specific for cells in S phase.
Mercaptopurine is used, usually with other agents, in
the treatment of leukaemia(the drug can be used in patients with acute
leukaemia cases in developed resistance to antifolievym drugs-methotrexate),
and worsening of chronic mieloleykoza. In addition, when used horionepiteliome
uterus (usually in combination with methotrexate) and the treatment
retikulezov. It induces remissions in acute lymphoblastic and myeloid
leukaemias but other agents are generally preferred and mercaptopurine is
chiefly employed in maintenance programmes, commonly with methotrexate. It may
also be effective in chronic myeloid leukaemia. There is cross-resistance
between mercaptopurine and tioguanine. Mercaptopurine has been used for its
immunosuppressant properties in the treatment of auto-immune disorders such as
inflammatory bowel disease but has been largely replaced by azathioprine.
It is also used for pediatric non-Hodgkin's lymphoma,
polycythemia vera, psoriatic arthritis, and inflammatory bowel disease (such as
Crohn's Disease and ulcerative colitis).
supplied: tablets 0,05 g.
ATC: L01BA01; L04AX03.
Methotrexate is an antineoplastic that acts as an
antimetabolite of folic acid. It also has immunosuppressant properties. Within
the cell, folic acid is reduced to dihydrofolic and then tetrahydrofolic acid.
Methotrexate competitively inhibits the enzyme dihydrofolate reductase and
prevents the formation of tetrahydrofolate which is necessary for purine and
pyrimidine synthesis and consequently the formation of DNA and RNA. It is most
active against cells in the S phase of the cell cycle.
Methotrexate is used in the management of acute
lymphoblastic leukaemia. It is seldom used for the induction of remission but
is employed in maintenance programmes and in the prophylaxis and treatment of
meningeal leukaemia. It may be used for Burkitt's and other non-Hodgkin's
lymphomas. In the solid neoplasms it is an important part of curative regimens
for choriocarcinoma and other gestational trophoblastic tumours, and for the
adjuvant therapy of osteosarcoma and breast cancer. It may also be used in
malignant neoplasms of the bladder and head and neck, and a variety of other
neoplasms, as indicated by the cross references given below.
Methotrexate is extensively used in the management of
malignant disease. In acute lymphoblastic leukaemia it is used for maintenance
therapy, and intrathecally for prophylaxis of CNS relapse, while it also forms
part of a number of regimens used for Burkitt's and other aggressive,
intermediate- to high-grade non-Hodgkin's lymphomas, including mycosis
fungoides and those associated with AIDS.
How supplied: film-coated tablets 0,0025 and 0,005 g.
Paclitaxel is a
taxane originally derived from the bark of the Pacific yew tree Taxus
brevifolia (Taxaceae), and now obtained semisynthetically from a taxane
precursor derived from the needles of the European yew, Taxus baccata.
Paclitaxel antineoplastic action arises from induction of microtubule formation
and stabilisation of microtubules, thereby disrupting normal cell division in
the G2 and M phases of the cell cycle.
used for the primary treatment of advanced ovarian cancer with cisplatin or
carboplatin, and for secondary treatment. In the treatment of node-positive
breast cancer, paclitaxel is used for primary adjuvant therapy after
anthracycline-containing chemotherapy. In locally advanced or metastatic breast
cancer, it is used first-line with an anthracycline, or as a second-line
single-agent, usually after failure of anthracycline-based therapy. In patients
with metastatic disease who overexpress HER2 (human epidermal growth receptor
2) it may be used with trastuzumab as initial therapy. Paclitaxel is used with
cisplatin or carboplatin, for the primary treatment of advanced non-small cell
lung cancer. It may be used for the second-line treatment of AIDS-related
Kaposi's sarcoma, and has been tried in a variety of other neoplasms including
cancers of the head and neck, and relapsed germ-cell tumours.
How supplied: concentrate for solution for infusion 0,6% (30 mg/5ml) in vials.
Tioguanine is an
analogue of the naturally occurring purine, guanine, and is an antineoplastic
with actions and uses similar to those of mercaptopurine. After incorporation
into DNA and RNA, the thio-group of tioguanine has a tendency to be methylated.
This leads to persistent 100-200 base single strand breaks. Such a genotoxic
stress will trigger cell cycle arrest and cell death. Tioguanine may be given
by mouth, usually with other antineoplastics, in the induction of remissions in
acute myeloid leukaemia (AML). It has also been used in other malignancies
including acute lymphoblastic leukaemia and chronic myeloid leukaemia, and
not effective in chronic lymphocytic leukemia, Hodgkin's lymphoma, multiple
myeloma, or solid tumors. Although thioguanine is one of several agents with
activity in the treatment of the chronic phase of chronic myelogenous leukemia.
How supplied: tablets 0,04 g.
INN: Zoledronic Acid
belongs to a group of drugs called bisphosphonates. Zoledronic acid also blocks
the osteoclastic resorption of mineralized bone and cartilage through its
binding to bone. Zoledronic acid inhibits the increased osteoclastic activity
and skeletal calcium release induced by various stimulatory factors released by
In the treatment
of skeletal complications from bone metastases secondary to multiple myeloma or
breast cancer, zoledronate was more effective than pamidronate in reducing the
risk of complications from breast cancer; it was of similar efficacy in those
with multiple myeloma. In a placebo-controlled trial in patients with prostate
cancer, zoledronate reduced the number of skeletal-related events, and
increased the median time to events. In patients with bone metastases arising
from lung cancer and other solid tumours (excluding breast or prostate cancer),
zoledronate reduced skeletal morbidity; the primary end-point, which excluded
hypercalcaemia as a skeletal-related event, did not reach statistical
significance. However, the authors noted that the patient groups had a shorter-than-expected
survival-time. A longer term follow-up of this study confirmed a sustained
reduction in risk of developing skeletal events with zoledronate. Whether
bisphosphonates can prevent the development of new skeletal metastases is
How supplied: Lyophilized powder for solution for infusion 0,004 g in vials.