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Biotech
Drugs
96
Biology
Graduate
05/01/2008

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Term
interferon alpha 2a, 2b, n1, n3
Definition
  • recombinant human interferon alpha
  • indicated for: hairy cell leukemia, AIDS-related Kaposi's sarcoma, chronic myelogenous leukemia, chronic hepatitis B and C, genital warts, papillomavirus
  • major adverse reactions: fever, myalgia and headache; flu like symptoms
Term
interferon alfacon-1
Definition
  • consensus alpha interferon, analog
  • indicated for: treatment of adult chronic hepatitis C
  • it was the first second generation interferon
  • side effects: flu-like symptoms, including fever, headache, myalgia, stiffness, fatigue
  • pts on long-term therapy suffer depression and irritability that can be severe
Term
peginterferon alpha 2a, 2b
Definition
  • pegylated recombinant human interferon alfa
  • indicated for: chronic hepatitis C alone or with ribavirin
  • pegylation allows once/week dosing
Term
interferon beta- 1b, 1a
Definition
  • recombinant human interferon beta
  • indicated for: relapsing, remitting multiple sclerosis and secondary progressive multiple sclerosis
  • Delivery: single-use, pre-filled syringes
  • adverse reactions: flu-like symptoms
Term
interferon gamma-1b
Definition
  • recombinant human interferon gamma
  • indications: reduces frequency/severity of infections associated with chronic granulomatous disease; delays disease progression in severe, malignant osteopetrosis
  • administered by subq injection 3x weekly at 50mcg/m2
Term

interferon drugs

(brand names)

Definition
  • Roferon-A
  • Intron A
  • Wellferon
  • Alferon N
  • Infergen
  • Pegasys
  • PEG-INTRON
  • Betaseron
  • Avonex, Rebif
  • Actimmune
Term

interferon drugs

(generic names)

Definition
  • Interferon alpha 2a, 2b, n1, n3
  • interferon alfacon-1
  • peginterferon alfa 2a, 2b
  • interferon beta- 1b, 1a
  • interferon gamma-1b
Term
Roferon-A
Definition
interferon alpha 2a
Term
Intron A
Definition
Interferon alpha 2b
Term
Wellferon
Definition
interferon alpha n1
Term
Alferon N
Definition
interferon alpha n3
Term
Infergen
Definition
interferon alfacon-1
Term
Pegasys
Definition
peginterferon alfa 2a
Term
PEG-INTRON
Definition
peginterferon alfa 2b
Term
Betaseron
Definition
interferon beta- 1b
Term
Avonex, Rebif
Definition
interferon beta- 1a
Term
Actimmune
Definition
interferon gamma-1b
Term

Interleukins and Regulators

(brand name)

Definition
  • Proleukin
  • Neumega
  • Kineret
Term
Interleukins and regulators
Definition
  • aldesleukin
  • oprelvekin
  • anakinra
Term
Aldesleukin
Definition
  • recombinant human interleuki-2
  • indications: metastatic malignant melanoma, metastatic renal cell carcinoma
  • severe toxicity inc. caplillary leak syndrome, cardiac arrythmias, angina, MI, respiratory failure, GI bleeding, and kidney failure
Term
Oprelvekin
Definition
  • thrombopoietic growth factor, IL-11
  • indications: prevention of chemotherapy-associated thrombocytopenia
  • 50mcg/kg SC every day for adults for 14-21 days
Term
Anakinra
Definition
  • selective interleukin-1 receptor antagonist
  • Indication: rheumatoid arthritis alone or with other DMARDs
  • 100mg/day SC; monitor neutrophil count for 3 months
Term

oligonucleotide drugs

(brand names)

Definition
  • Vitavene
  • Macugen
Term

oligonucleotide drugs

(generic names)

Definition
  • fomivirsen sodium
  • pegaptanib sodium
Term
Types of oligonucleotide drugs
Definition
  • antisense
  • siRNA
  • aptamers
Term
Fomivirsen Sodium
Definition
  • structure: 21-base phosphorothionate oligonucleotide
  • indications: cytomegalovirus retinitis in HIV pts intolerant or nresponsive to other approved treatments
  • 1st FDA approved, believed to act by an antisense mechanism (blocking synthesis of the CMV immediate early protein 1E2), it is no suspected to act as an interferon inducer
  • injected directly into the vitreous eye fluid
Term
Follistim
Definition
Follitropin beta
Term
Vitravene
Definition
fomivirsen sodium
Term
pegaptanib sodium
Definition
  • pegylated 28-mer oligonucleotide
  • indication: neovascular (wet) age-related macular degeneration
  • first aptamer drug, which binds to and inactivates extracellular VEGF
  • injected directly into the vitreous fluid of the eye
Term
Macugen
Definition
pegaptanib sodium
Term
etanercept
Definition
  • dimeric fusion protein of TNF-alpha receptor + IgG1 Fc
  • Indication: reduce signs and symptoms of ankylosing spondylitis; plaque psoriasis; psoriatic arthritis; adult and juvenile RA alone and with methotrexate
  • not to be used in patients with serious infection or sepsis; cost $10,400/yr
Term
enbrel
Definition
etanercept
Term

Pseudoantibodie drugs

(generic names)

Definition
  • etanercept
  • alefacept
  • abatacept
Term

pseudoantibody drugs

(brand name)

Definition
  • Enbrel
  • Amevive
  • Orencia
Term
alefacept
Definition
specificity: CD-2 receptor
Term
abatacept
Definition
specificity: T-cell antigen 4 sites
Term
Amevive
Definition
alefacept
Term
Orencia
Definition
abatacept
Term
Gemtuzumab ozogamicin
Definition
  • humanized monoclonal ab against CD33 attached to calicheamicin via a thiol-cleavable linker
  • indication: CD-33 positive acute myeloid leukemia
  • first immunotoxin approved; calicheamicin is a far too cytotoxic antibody to be useful in cancer chemotherapy on its own
Term
Mylotarg
Definition
gemtuzumab ozogamicin
Term

denileukin difitox

Definition
  • diptheria toxin fragments A and B fused to an interleukin-2 fragment
  • Indication: CD25 positive persistent/recurrent cutaneousT-cell lymphoma
  • first fusion toxin to be approved; its an orphan drug costing $25-50 thous. per treatment
Term
Ontak
Definition
denileukin difitox
Term

Interleukin drugs

(brand name)

Definition
  • Proleukin
  • Neumega
  • Kineret
Term

Interleukin drugs

(generic name)

Definition
  • aldesleukin
  • oprelvekin
  • anakinra
Term

Colony stimulating factor drugs

(generic names)

Definition
  • Filgrastim
  • Pegfilgrastim
  • sargramostim
Term

Colony stimulating factor drugs

(brand name)

Definition
  • Neupogen
  • Neulasta
  • Leukine/Prokine
Term
aldesleukin
Definition
IL-2
Term
Oprelvekin
Definition
IL-11
Term
Anakinra
Definition
IL-1 antagonist
Term
filgrastim
Definition
stimulates neutrophil production
Term
pegfilgrstim
Definition
  • stimulates neutrophil production, but has a longer half life than filgrastim
  • pegylated filgrastim
  • indication: decreases chemotherapy-associated neutropenia
  • modified filgrastim with lower clearance rates and increased circulation lifetimes
Term
sargramostim
Definition
stimulates granulocyte and macrophage production
Term

coagulation factor drugs

(generic name)

Definition
  • moroctocog alfa
  • eptacog alfa
  • nonacog alfa
Term

coagulation factor drugs

(brand name)

Definition
  • Helixate-P/ Kogenate/ Recombinate/ Refacto/ Advate/ Bioclate
  • NovoSeven
  • BeneFIX
Term
Moroctocog alfa
Definition
Factor VIII
Term
eptacog alfa
Definition
Factor VIIa
Term
Nonacog
Definition
Factor IX
Term

Growth factors turned into drugs

(generic names)

Definition
  • becaplermin
  • palifermin
  • Bone morphogenic protein-2
Term

Growth factors turned into drugs

(brand name)

Definition
  • Regranex Gel
  • Kepivance
Term
Regranex Gel
Definition
Becaplermin
Term
Kepivance
Definition
Palifermin
Term
becaplermin
Definition
  • indication: diabetic ulcers of the lower limbs and feet that extend into the subcutaneous layer or beyond
  • recombinant B chain of the homodimer of human platelet-derived growth factor synthesized in Sacchromyces cerevisiae (yeast)
  • PDGF stimulates mitosis and movement offibroblasts, neutrophils and macrophages, which are all involved in tissue repair.Fibroblasts stimulated to secrete collagenase, which is used in tissue remodeling (stage in wound healing)
Term
pilfermin
Definition
  • indication: reduces the chances of developing severe mucositis (injury to the cells lining the mouth) and shortening recovery time from severe mucositis in patietns with cancer who recive high doses of chemotherapy and radiation therapy followed by stem cell rescue
  • recombinant human keratinocyte growth factor, which stimulates the growth of cells in tissue such as skin and the surface layer of the mouth, stomach lining, and colon
Term
Bone Morphogenic Protein-2
Definition
  • indication: spinal fusion procedures in skeletally mature pts with degenerative disc disease
  • Marketed by Medtronic
  • BMP-2 is produced in E.coli at Wyeth
  • signaling for osteogenesis occurs through receptor serine threonine kinases
Term
Superovulation Hormones for In Vitro Fertilization
Definition
  • Follicle Stimulating Hormone:
    • Follitropin alfa (Gona-F)
    • Follitropin beta (Follistim)
  • Luteinizing hormone:
    • Lutropin alfa (Luveris)
  • Human choriogonadotropin:
    • Choriogonadotropin alfa (Ovidrel)
Term
Gonal-F
Definition
Follitropin alfa
Term
Ovidrel
Definition
Choriogonadotropin alfa
Term
Luveris
Definition
Lutropin alfa
Term
Glucagon
Definition
Use: acute hypoglycemia
Term
Thyroid-stimulating hormone
Definition
thyrotropin alfa (Thyrogen)
Term
Thyrogen
Definition
Thyrotropin alfa
Term
thyrotropin alfa
Definition
use: thyroid cancer diagnosis
Term
Atrial Natriuetic Factor
Definition
Nesirtide (Natrecor)
Term
Nesiritide
Definition
use: congestive heart failure
Term
Natrecor
Definition
Nesiritide
Term
Parathyroid hormone
Definition
teriparatide (Forteo)
Term
Teriparatide
Definition
use: osteoporosis
Term
Forteo
Definition
teriparatide
Term
Drotrecogin alfa
Definition
  • activatedprotein C acute phase protein
  • indication: severe sepsis associated with organ dysfunction and high risk of death
  • binds to high affinity interleukin-2 receptor on activated Thelper cells
  • acute phase proteins produced by body in response to infection, and are normally purified from pleural fluid
  • sepsis is the leading cause of bankruptcy in biotech companies
Term
Xigris
Definition
drotrecogin alfa
Term
Short interfering RNA (siRNA)
Definition
  • no FDA approved drugs yet
  • most research for oligonucleotide drugs is aimed at exploiting natural mechanism that specifically turns off protein synthesis with oligonucleotides
  • short interfering RNA turns out to work much better than antisense with RNAse H- typically siRNA 10 to 200 x more active
Term
Abciximab
Definition
  • chimeric Fab fragment that binds to glycoprotein IIb/IIIa receptor of platelets blocking aggregation
  • indications: adjunct to angioplasty (PCI); unstable angina during PCI, MI
  • contraindicated for major surgery, trauma or other bleeding risk within 6 weeks
Term
ReoPro
Definition
Abciximab
Term
Alteplase
Definition
  • human tissue plasminogen activator (tPA, an enzyme

indication: acute MI, stroke, and pulmonary embolism

causes clot lysis by converting plasminogen into plasmin by limited proteolysis. It binds to fibrin in blood clots, and is activated 400x, allowing it to preferentially lyse clots with limited systemic proteolysis 

Term
Activase
Definition
Alteplase
Term
Reteplase
Definition
  • second generation thrombolytic
  • contains only 2 of the domain: protease and kringle-2. since it is smaller it will diffuse faster.
Term
Tenecteplase
Definition
  • the same as alteplase but has 6 amino acid substitutions specifically designed to prolong its half-life, enabling single bolus dosing, and increased specificity for fibrin
  • substitution of threonine 103 w/ asp, asp117 w/ glu, and amino acids 296-299 with tetr-alanine
  • results in less disturbance of the coagulation system
Term
Neulasta
Definition
pegfilgrastim
Term
Pegvisomant
Definition
  • pegylated analog of human growth hormone
  • indication: acromegaly
  • 1st GH receptor antagonist produced: contains 191 amino acid residues to which 4-6 PEG polymers are covalently bound
Term
Somavert
Definition
pegvisomant
Term
Methoxypolyethyleneglycol epoetin beta
Definition
  • pegylated erythropoietin
  • indication: treatment of anemia associated with chronic kidney disease
  • allows once per month dosing
Term
Mircera
Definition
methoxypolyethyleneglycol epoetin beta
Term
epoetin alfa
Definition
  • cytokine that stimulates red blood cell production
  • indication: anemia in chemotherapy and AZT Tx, chronic renal failure; reduces red blood transfusions in surgery
  • first biotechnology blockbuster with US sales >$1 billion/yr;potential drug of abuse in endurance athletes
Term
Epogen
Definition
epoetin alfa
Term
Darbepoetin
Definition
  • second generation erythropoetin
  • highly sialylated EPO
  • indication: anemia in chronic renal failure, chronic renal insufficiency and chemotherapy
  • Darbepoetin achieves a 3x longer circulating half-life due to increased sialylation
Term
Aranesp
Definition
Darbepoetin
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