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 To define the target treatment groups:  Monoclonal  Cancer vaccines  TKI  Hematopoetic growth factors

 To Know the indication, contraindication and Drug-Drug interactions of each target treatment group.

Monoclonal Antibodies Approved by the EMA and FDA for Therapeutic Use (status 2013)

Drug Name Target Therapeutic Indications Muromonab CD3 Transplantation rejection Satumomab TAG-72 Detection of colorectal and ovarian cancers (non-therapeutic) Nofetumomab Carcinoma- Diagnostic imaging of small-celllung cancer associated (non-therapeutic) Capromab Tumor surface Detection of prostate adenocarcinoma antigen PSMA (non-therapeutic) Arcitumomab Human CEA Detection of colorectal cancer (non-therapeutic) antigen - CD25 (a chain of Reversal of transplantation rejection - IL2 receptor) Drug Name Target Therapeutic Indications CD20 Non-Hodgkin’s , Chronic lymphocytic , Rheumatoid arthritis HER-2 Breast cancer, Metastatic gastric or gastro esophageal junction, adenocarcinoma Gemtuzumab CD33 Acute myeloic leucemia (AML) ozogamicin Ibritumomab CD20 Non-Hodgkin’s lymphoma tiuxetan CD52 B-cell chronic lymphocytic leukemia

Bevacizumab VEGF Metastatic colorectal cancer, Non-small cell , Metastatic breast cancer, Glioblastoma multiforme , Metastatic renal cell carcinoma EGFR Head and neck cancer, Colorectal cancer

Panitumumab EGFR Metastatic colorectal carcinoma Drug Name Target Therapeutic Indications

Eculizumab Complement C5 Paroxysmal nocturnal hemoglobinuria

-Trastuzumab HER2 Breast cancer emtansine -

- CD20 CLL -

Brentuximab CD30 Hodgkin lymphoma (HL), systemic anaplastic large cell lymphoma (ALCL)

Ipilimumab CTLA-4

Denosumab RANKL Prevention of SREs in patients with bone metastases from solid tumours Drug Name Target Therapeutic Indications

Abciximab GPIIb/IIIa High risk angioplasty(prevention of blood clots)

Imiciromab Human cardiac Myocardial infarction imaging agent (non- myosin therapeutic)

Sulesomab NCA90 Diagnostic imaging forosteomyelitis (non- therapeutic0

Infliximab TNFα Crohn’s diseaseUlcerative colitis, Rheumatoid arthritisAnkylosing spondylitis ,Psoriatic arthrits Plaque psoriasis Palivizumab F-protein of RS Respiratory Syncytial Virus (RSV) virus Votumumab Cytokeratintumo Detection of carcinoma of thecolon or rectum r-associated (non-therapeutic) antigen Drug Name Target Therapeutic Indications

Adalimumab TNFα Rheumatoid arthritis, Juvenile idiopathic arthritis, Psoriatic arthritis, Ankylosing spondylitis ,Crohn’s disease, Plaque psoriasis CD11a Psoriasis

Omalizumab IgE Asthma

Tositumomab CD20 Non-Hodgkin’s lymphoma and iodine 131 Fanolesomab CD15 Imaging of equivocal appendicitis (non- therapeutic) VLA-4 Multiple sclerosis (relapsing)Crohn’s disease Drug Name Target Therapeutic Indications

Catumaxomab EpCAM Head and neck cancer

Ranibizumab VEGF-A Neovascular (wet) age-related macular degeneration, Macular edema following retinalvein occlusion Certolizumab TNFa Crohn’s diseaseRheumatoid arthritis pegol

Canakinumab IL-1ß Cryopyrin-associated periodic syndromes, including familial cold autoinflammatory syndrome and Muckle-Wells syndrome EpCAM and Malignant ascites in patients with EpCAM-positive CD3 carcinomas TNFa Rheumatoid arthritisPsoriatic, arthritisAnkylosing spondylitis Drug Name Target Therapeutic Indications

Tocilizumab IL-6 receptor Rheumatoid arthritis

Ustekinumab IL-12 / IL-23 Plaque psoriasis

Besilesomab NCA-95 Diagnosis of inflammation / infection sites via scintigraphic imaging (non-therapeutic)

Belimumab BLyS Systemic lupus erythematosus (SLE)

Raxibacumab Bacillus anthracis Prevention and treatment of inhalation anthrax protective antigen Contraindications / Cautions

 caution in elderly patients  caution if cardiovascular disease or history  caution if angina or history  caution if pulmonary disease  caution if high tumor burden  caution if HBV carrier  caution if infection, latent or chronic

Types of Cancer Vaccines

Preventive or Prophylactic

• HPV • HBV

Treatment

• For metastatic prostate cancer What cancer preventive vaccines are approved FDA?

 Human papillomavirus (HPV) vaccines. Persistent infections with high risk HPV types can cause cervical cancer, anal cancer, orpharyngeal cancer, and vaginal, vulvar, and penile cancers.

Three vaccines are approved by the US (FDA) to prevent HPV infection: • Gardasil • Gardasil 9 • Cervarix What cancer preventive vaccines are approved FDA?

 Hepatitis B virus (HBV) vaccines. Chronic HBV infection can lead to Liver cancer.

Two vaccines are approved by the US (FDA) to prevent HBV infection: • Engerix-B • Recombivax HB Active Clinical Trials of Cancer Active Clinical Trials of Cancer Treatment Vaccines by Type of Preventive Vaccines by Type of Cancer: Cancer:

•Lung Cancer •Cervical Cancer •Non-Hogkin Lymphoma •Solid Tumors •Prostate Cancer •Breast Cancer •Bladder Cancer •Brain Cancer •Ovarian Cancer •Solid Tumor •Pancreatic Cancer •Multiple Myloma •Melanoma •Leukemia Contraindications for Adult Vaccine:

• Hepatitis B vaccine: Sensitivity to yeast.

• HPV vaccine: Pregnancy and anaphylactic shock to previous dose. is a therapeutic for the treatment of solid tumors that is currently under clinical development by Recombio, an international public-private consortium with the participation of the Center of Molecular Immunology at Havana, Cuba (CIM) and researchers from Buenos Aires University and National University Of Quilmes In .

Racotumomab triggers an immune response against the tumor antigen N-glycolil (NGcGM3), a type of ganglioside present on the cell surface of malignant cells from lung and breast, melanoma.

Racotumomab is administered in patients who have previously received the oncospecific treatment established in the oncological therapeutic standards (surgery, and ). A Racotumomab solution is administered by intradermal injection every 14 days for the first 2 months (5 doses), followed by monthly booster doses.

Racotumomab has been approved in two countries, Argentina and Cuba, for the treatment of recurrent or advanced NSCLC, or NSCLC independent of the disease stage when no other standard therapy can be administered.

(FDA)-Approved Tyrosine Kinase Inhibitors (TKIs)

Drug Name Target Therapeutic Indications

Dasatinib BCR-ABL, SRC Chronic myeloid leukemia, acute lymphocytic (Sprycel) family, c-KIT, leukemia PDGFR (Tarceva) EGFR Non-small cell lung cancer, pancreatic cancer

Gefitinib (Iressa) EGFR Non-small cell lung cancer

Imatinib (Gleevec) BCR-ABL, Acute lymphocytic leukemia, chronic myeloid c-KIT, leukemia, gastrointestinal stromal tumors, PDGFR hypereosinophilic syndrome, systemic mastocytosis

(FDA)-Approved Tyrosine Kinase Inhibitors (TKIs)

Drug Name Target Therapeutic Indications

Lapatinib (Tykerb) HER2/neu, Breast cancer with HER2/neu overexpression EGFR (Tasigna) BCR-ABL, c- Chronic phase or accelerated Ph- positive CML for KIT, PDGFR patients resistant/intolerant of prior therapy

Sorafenib (Nexavar) BRAF,VEGF Renal cell cancer, hepatocellular carcinoma REGFR,PD GFR (Sutent) VEGFR,PD Renal cell cancer, gastrointestinal stromal tumor GFR, c- KIT,FLT3 Drug interactions with the tyrosine kinase

Available HGFs are:

G-CSF GM-CSF TPO EPO CSF Therapeutic Indications

• EPO was beneficial in raising the hemoglobin levels of patients with MDS. Also, EPO is more likely to be useful in nontransfused anemic patients as opposed to those who have already begun transfusions.

• G-CSF or GM-CSF to increase the absolute neutrophil count of neutropenic patients with MDS, have a special role in the setting of bone marrow transplantation (BMT).

• In leukemic patients, CSFs have been used to prime patients, theoretically lining up blasts in the same cell phase so that chemotherapy will be more effective.

• TPO mimetics (romiplostim and eltrombopag) have demonstrated efficacy in raising platelet counts in ITP patients. They have been used in both pre and postsplenectomy patients.

Other Types of Biotherapy: ( and )

Interleukins Principal Source Primary Activity

co-stimulation of APCs and T cells, and other antigen presenting cells IL1-α and -β inflammation and fever, acute phase (APCs) response, hematopoiesis

proliferation of B cells and activated T IL-2 activated Th1 cells, NK cells cells, NK functions

growth of hematopoietic progenitor IL-3 activated T cells cells

B cell proliferation, eosinophil and mast cell growth and function, IgE and IL-4 Th2 and mast cells class II MHC expression on B cells, inhibition of monokine production

IL-5 Th2 and mast cells eosinophil growth and function Interleukins Principal Source Primary Activity

hematopoietic and thymopoietic IL-9 T cells effects

synergisitc hematopoietic and IL-11 bone marrow stromal cells thrombopoietic effects

regulates the growth and IL-14 T cells and malignant B cells proliferation of B cells

eosinophils, CD8+ T cells, lymphocytes, IL-16 chemoattractant for CD4+ cells epithelial cells

antiviral effects, induction of class macrophages, neutrophils and some I MHC on all somatic cells, INF-α and -β somatic cells activation of NK cells and macrophages

Hormone Therapy

Hormone Therapy for Breast Cancer

 Some types of breast cancer are affected by hormones in the blood. ER-positive and PR-positive breast cancer cells have receptors that attach to estrogen, which helps them grow. There are different ways to stop estrogen from attaching to these receptors.  Hormone therapy is a form of systemic therapy, meaning it reaches cancer cells anywhere in the body and not just in the breast. It's recommended for women with hormone receptor-positive (ER-positive and/or PR-positive) breast cancers, but it does not help women whose tumors are hormone receptor-negative (both ER- and PR-negative).

Treatments that lower estrogen levels

 Aromatase inhibitors (AIs) are drugs that stop estrogen production.  Letrozole (Femara)  Anastrozole (Arimidex)  Exemestane (Aromasin) Drugs that block estrogen receptors

 Tamoxifen; This drug blocks estrogen receptors in breast cancer cells.  Toremifene (Fareston) is another SERM that works in a similar way, but it is used less often and is only approved to treat metastatic breast cancer.  Fulvestrant is a drug that blocks estrogen receptors and also eliminates them temporarily.

Ovarian ablation

 For pre-menopausal women, removing or shutting down the ovaries (ovarian ablation), which are the main source of estrogens, effectively makes them post-menopausal. This may allow some other hormone therapies, such as AIs, to work better.  Oophorectomy: Surgery is done to remove the ovaries. This is a form of permanent ovarian ablation.  Luteinizing hormone-releasing hormone (LHRH) analogs: These drugs are used more often than oophorectomy. They stop the signal that the body sends to ovaries to make estrogen, which causes temporary menopause. Less common types of hormone therapy  Some other types of hormone therapy were used more often in the past, but are rarely given now. These include:  Megestrol acetate (Megace), a progesterone-like drug  Androgens (male hormones)  High doses of estrogen  These might be an option if other forms of hormone therapy are no longer working, but they can often cause side effects.

Hormone Therapy for Prostate Cancer

 Hormone therapy is also called androgen deprivation therapy (ADT) or androgen suppression therapy.  Luteinizing hormone-releasing hormone (LHRH) agonists (also called LHRH analogs or GnRH agonists) are drugs that lower the amount of testosterone made by the testicles. Treatment with these drugs is sometimes called chemical castration or medical castration because they lower androgen levels just as well as orchiectomy.  Leuprolide (Lupron, Eligard)  Goserelin (Zoladex)  Triptorelin (Trelstar)  Histrelin (Vantas)

Hormone Therapy for Prostate Cancer  LHRH antagonist  Degarelix (Firmagon) is an LHRH antagonist.  CYP17 inhibitör  LHRH agonists and antagonists can stop the testicles from making androgens, but other cells in the body, including prostate cancer cells themselves, can still make small amounts, which can fuel cancer growth. Abiraterone (Zytiga) blocks an enzyme called CYP17, which helps stop these cells from making androgens. Hormone Therapy for Prostate Cancer  Drugs that stop androgens from working  Anti-androgens Androgens have to bind to a protein in the prostate cell called an androgen receptor to work. Anti-androgens are drugs that bind to these receptors so the androgens can’t. Flutamide (Eulexin) Bicalutamide (Casodex) Nilutamide (Nilandron)  They are taken daily as pills.  Enzalutamide (Xtandi) is a newer type of anti-androgen

Hormone Therapy for Prostate Cancer  Estrogens (female hormones) were once the main alternative to orchiectomy for men with advanced prostate cancer.  Ketoconazole (Nizoral), first used for treating fungal infections, blocks production of certain hormones, including androgens, much like abiraterone. It's most often used to treat men just diagnosed with advanced prostate cancer who have a lot of cancer in the body, as it offers a quick way to lower testosterone levels. It can also be tried if other forms of hormone therapy are no longer working. References:

 http://onlinelibrary.wiley.com/doi/10.3322/canjclin.46.3.165/full

 http://www.clevelandclinicmeded.com/medicalpubs/diseasemanagem ent/hematology-/use-of-hematopoietic-growth-factors/#top

 https://www.cancer.gov/about-cancer/causes-prevention/vaccines- fact-sheet

 http://www.vaxira.com/en_vaxira.html#supervivenciaGlobal

 https://www.oncolink.org/cancer-treatment/therapies/targeted/part- one-introduction-to-small-molecule-tyrosine-kinase-inhibitors