Miomio, Juliet Marie L.

BSN-2D NCM 109

List down and define all the pharmacological medication for chemotherapy and radiation
therapy. Include the mechanism of action.

1. Omacetaxine- A cephalotaxine used in the treatment of Chronic Myeloid

Leukemia (CML) that is intolerant to or resistant to two or more tyrosine kinase
inhibitors.

Brand Names: Synribo

Generic Name: Omacetaxine mepesuccinate

Indication: Used in patients who are intolerant and/or resistant to two or more tyrosine
kinase inhibitors used to treat accelerated or chronic phase CML.

Mechanism of Action: Homoharringtonine inhibits protein synthesis by not directly

binding to Bcr-Abl. It binds to the A-site cleft in the large ribosomal subunit, which
affects chain elongation and prevents protein synthesis.

2. Dacarbazine- An antineoplastic agent used to treat malignant melanoma and

Hodgkin's disease.
Generic Name: Dacarbazine
Indication: For the treatment of metastatic malignant melanoma. In addition,
dacarbazine is also indicated for Hodgkin's disease as a secondary-line therapy when
used in combination with other antineoplastic agents.
Mechanism of Action: Appears to exert cytotoxic effects via its action as an alkylating
agent. Other theories include DNA synthesis inhibition by its action as a purine analog,
and interaction with SH groups. Dacarbazine is not cell cycle-phase specific.

3. Ifosfamide- An alkylating and immunosuppressive agent used in chemotherapy

for the treatment of cancers, including testicular cancer, ovarian cancer, cervical
cancer, osteocarcinoma, bladder cancer, small cell lung cancer, and non-
Hodgkin's lymphoma.
Brand Names: Ifex Generic Name: Ifosfamide
Indication: Used as a component of various chemotherapeutic regimens as third-line
therapy for recurrent or refractory germ cell testicular cancer. Also used as a component
of various chemotherapeutic regimens for the treatment of cervical cancer, as well as in
conjunction with surgery and/or radiation therapy in the treatment of various soft tissue
sarcomas
Mechanism of Action: The exact mechanism of ifosfamide has not been determined,
but appears to be similar to other alkylating agents. Ifosfamide requires
biotransformation in the liver by mixed-function oxidases (cytochrome P450 system)
before it becomes active.

4. Altretamine- An antineoplastic agent used in palliative treatment of persistent or

recurrent ovarian cancer.
Generic Name: Altretamine
Indication: Use as a single agent in the palliative treatment of patients with persistent
or recurrent ovarian cancer.
Mechanism of Action: Altretamine exerts its cytotoxic effect is unknown although it is
classified as an alkylating anti-neoplastic agent. Through this mechanism, the drug is
metabolized into alkylating agents by N-demethylation.

5. Procarbazine- An antineoplastic agent indicated for the treatment of stage III

and stage IV Hodgkin's disease in combination with other chemotherapeutic
agents.
Brand Names: Matulane Generic Name: Procarbazine
Indication: For use with other anticancer drugs for the treatment of stage III and stage
IV Hodgkin's disease.
Mechanism of Action: The precise mode of cytotoxic action of procarbazine has not
been clearly defined. There is evidence that the drug may act by inhibition of protein,
RNA and DNA synthesis. Studies have suggested that procarbazine may inhibit
transmethylation of methyl groups of methionine into t-RNA.

6. Cyclophosphamide- A nitrogen mustard used to treat lymphomas, myelomas,

leukemia, mycosis fungoides, neuroblastoma, ovarian adenocarcinoma,
retinoblastoma, and breast carcinoma.
Brand Names: Procytox
Generic Name: Cyclophosphamide
 Indication: Cyclophosphamide is indicated for the treatment of malignant lymphomas,
multiple myeloma, leukemias, mycosis fungoides (advanced disease), neuroblastoma
(disseminated disease), adenocarcinoma of the ovary, retinoblastoma, and carcinoma
of the breast.
Mechanism of Action: Attachment of alkyl groups to DNA bases, resulting in the DNA
being fragmented by repair enzymes in their attempts to replace the alkylated bases,
preventing DNA synthesis and RNA transcription from the affected DNA, DNA damage
via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA
from being separated for synthesis or transcription, and the induction of mispairing of
the nucleotides leading to mutations.

7. Bendamustine- An antineoplastic agent used for the treatment of chronic

lymphocytic leukemia (CLL) and indolent B-cell non-Hodgkin lymphoma (NHL)
that has progressed following rituximab therapy.
Brand Names: Belrapzo, Bendek, Treanda Generic Name: Bendamustine
Indication: Indicated for use in the treatment of chronic lymphocytic leukemia (CLL)
and indolent B-cell non-Hodgkin lymphoma (NHL) that has progressed during or within
six months of treatment with rituximab or a rituximab-containing regimen.
Mechanism of Action: A bifunctional mechlorethamine derivative capable of forming
electrophilic alkyl groups that covalently bond to other molecules. Through this function
as an alkylating agent, bendamustine causes intra- and inter-strand crosslinks between
DNA bases resulting in cell death.

8. Pegaspargase- A modified form of L-asparagine amidohydrolase used to treat

acute lymphoblastic leukemia, which is dependent on an external source of
asparagine.
Brand Names: Oncaspar Generic Name: Pegaspargase
Indication: For treatment of acute lymphoblastic leukemia
Mechanism of Action: It facilitates production of oxaloacetate which is needed for
general cellular metabolism. Some malignant cells lose the ability to produce
asparagine and so the loss of exogenous sources of asparagine leads to cell death.

9. Busulfan- An alkylating agent used to treat chronic myelogenous leukemia.

Brand Names: Busilvex, Busulfex, Myleran Generic Name: Busulfan
Indication: For use in combination with cyclophosphamide as a conditioning regimen
prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous
(myeloid, myelocytic, granulocytic) leukemia (FDA has designated busulfan as an
orphan drug for this use). It is also used as a component of pretransplant conditioning
regimens in patients undergoing bone marrow transplantation for acute myeloid
leukemia and nonmalignant diseases.
Mechanism of Action: Busulfan is an alkylating agent that contains 2 labile
methanesulfonate groups attached to opposite ends of a 4-carbon alkyl chain. Once
busulfan is hydrolyzed, the methanesulfonate groups are released and carbonium ions
are produced.

10. Lomustine- An alkylating agent used as a part of chemotherapeutic regimens for

the treatment of primary and metastatic brain tumors as well as refractory or
relapsed Hodgkin's disease in addition to surgical and/or radiotherapeutic
treatments.
Brand Names: Ceenu, Gleostine Generic Name: Lomustine
Indication: For the treatment of primary and metastatic brain tumors as a component of
combination chemotherapy in addition to appropriate surgical and/or radiotherapeutic
procedures. Also used in combination with other agents as secondary therapy for the
treatment of refractory or relapsed Hodgkin's disease.
Mechanism of Action: Lomustine is a highly lipophilic nitrosourea compound which
undergoes hydrolysis in vivo to form reactive metabolites. These metabolites cause
alkylation and cross-linking of DNA (at the O6 position of guanine-containing bases) and
RNA, thus inducing cytotoxicity.

Radiation Therapy Medication

11. Bevacizumab- A monoclonal anti-vascular endothelial growth factor antibody

used in combination with antineoplastic agents for the treatment of many types of
cancer.
Brand Names: Avastin, Mvasi Generic Name: Bevacizumab
Indication: As a vascular endothelial growth factor (VEGF) inhibitor, bevacizumab is
used in several chemotherapy regimens to treat metastatic colorectal cancer;
metastatic, unresectable, locally advanced or recurrent non-squamous non-small cell
lung cancer; metastatic renal cell carcinoma; metastatic, persistent, or recurrent cervical
cancer; primary peritoneal cancer; epithelial ovarian cancer; and fallopian tube cancer.
It can also be used to treat recurrent glioblastoma
Mechanism of Action: induced by 'hypoxia inducible factor' (HIF) in a hypoxic
environment. When circulating VEGF binds to VEGF receptors (VEGFR-1 and VEGFR-
2) located on endothelial cells, various downstream effects are initiated. It should be
noted that VEGF also binds to the neuropilin co-receptors (NRP-1 and NRP-1), leading
to enhanced signaling.

12. Panitumumab- A recombinant humanized monoclonal antibody used to treat

EGFR-expressing, metastatic colorectal carcinoma that is refractory to
fluoropyrimidine-, oxaliplatin-, and irinotecan- containing chemotherapy
regimens.
Brand Names: Vectibix Generic Name: Panitumumab
Indication: For the treatment of EGFR-expressing, metastatic colorectal carcinoma that
is refractory to fluoropyrimidine-, oxaliplatin-, and irinotecan- containing chemotherapy
regimens.
Mechanism of Action: Panitumumab binds specifically to EGFR on both normal and
tumor cells, and competitively inhibits the binding of ligands for EGFR. Nonclinical
studies show that binding of panitumumab to the prevents ligand-induced receptor
autophosphorylation and activation of receptor-associated kinases, resulting in inhibition
of cell growth, induction of apoptosis, decreased pro-inflammatory cytokine and
vascular growth factor production, and internalization of the EGFR.

13. Trastuzumab- A monoclonal anti-human epidermal growth factor receptor 2

protein antibody used to treat HER2-positive breast, gastroesophageal, and
gastric cancers.
Brand Names: Herceptin, Herceptin Hylecta, Herzuma Generic Name: Trastuzumab
Indication: As part of a treatment regimen consisting of doxorubicin,
cyclophosphamide, and either paclitaxel or docetaxel; as part of a treatment regimen
with docetaxel and carboplatin; or as monotherapy following multi-modality
anthracycline-based therapy.
Mechanism of Action: Trastuzumab is a recombinant humanized IgG1 monoclonal
antibody against the HER-2 receptor, a member of the epidermal growth factor
receptors which is a photo-oncogene. Over-expressed in breast tumour cells, HER-2
overamplifies the signal provided by other receptors of the HER family by forming
heterodimers.
 14. Erlotinib- An EGFR tyrosine kinase inhibitor used to treat certain small cell lung
cancers or advanced metastatic pancreatic cancers.
Brand Names: Tarceva Generic Name: Erlotinib
Indication: The treatment of metastatic non-small cell lung cancer (NSCLC) with
tumors showing epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21
(L858R) substitution mutations Label. In combination with first-line treatment for patients
diagnosed with locally advanced, unresectable or metastatic pancreatic cancer.
Mechanism of Action: Erlotinib inhibits the intracellular phosphorylation of tyrosine
kinase associated with the epidermal growth factor receptor (EGFR).