PHRM30003 Study Guide - Final Guide: Rituximab, Mast Cell, Melanoma
5 Jun 2018
School
Department
Course
Professor
Drug name
Drug class
Molecular target(s)
Mechanism
/Function
Contradiction
/
AE/
Notes
Immunosuppressants
(4)
–
used in combination to reduce AE
Cyclosporin
Calcineurin
inhibitor
Cyclophilin
(Immunophilin)
Inhibit calcineurin
inside T cell
Decrease dephosphorylated NFAT
Decrease transcription of IL-2
Decrease T cell proliferation
Discovered by random screening
from soil
fungus
AE: Nephrotoxicity - kidney
Tacrolimus
Calcineurin inhibitor
FKBP
(Immunophilin)
Inhibit calcineurin inside T cell
Decrease dephosphorylated NFAT
Decrease transcription of IL-2
Decrease T cell proliferation
Similar to Cyclosporin
AE:Nephrotoxicity
Sirolimus
(Rapamycin)
Calcineurin
inhibitor
(?)
FKBP
(Immunophilin)
Inhibit
mTOR
Decrease T cell proliferation
No effect on calcineurin
AE: Hyperlipidaemia – liver
Methylprednisolone
GCs
With high systemic conc
AE: Increase risk of asthma
Mycophenolate
mofetil
Azathioprine
Cytotoxic drugs
Anti-metabolites
Inhibits purine
synthesis
More selective toward lymphocytes
So decrease T cell proliferation
Also anti
-
cancer
Muromona
b
mAb/Biologicals
CD3
Depletion of lymphocytes
:
ADCC, CDC, apoptosis
Blockade/loss of activating receptors
Increased risk of infection
Cancer
Basiliximab
mAb/Biologicals
IL
-
2R = CD25
Depletion of lymphocytes:
ADCC, CDC, apoptosis
Blockade/loss of activating receptors
Increased risk of infection
Cancer
Daclizamab
mAb/biologicals
IL
-
2R = CD25
Depletion of lymphocytes:
ADCC, CDC, apoptosis
Blockade/loss of activating receptors
Increased risk of infection
Cancer
Belatacept
Abatacept
mAb/biologicals
B7 = CD80/86
Avoid B7 binds to CD28 to trigger T cell
proliferation
CD28 (+)
Immunostimulants
(3)
Ipilimumab
Anti
-
cancer
m
Ab
CTLA4(
-
)
Co-stimulatory
Avoid B7 binds to CTLA4 to dampen T cell
expansion
Depletion of lymphocytes:
ADCC, CDC, apoptosis
Blockade/loss of activating receptors
CTLA4 inhibits T cell response
Nivolumab
Pembrolizumab
Anti
-
cancer
m
Ab
PD1(
-
)
Co-stimulatory
Depletion of lymphocytes:
ADCC, CDC, apoptosis
PD1 inhibit
s
T cell response
