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Pharmacology

• Anticancer drugs

Lecture No.-2 Dr Ankit Kumar (MD, DM)


1 Cytotoxic drugs

2 Targeted therapy
Purine analogue
1. 6 Thioguanine
} guanine Analogue
2. 6 Mercaptopurine

3. Cladribine
4. Fludarabine Adenine Analogue.

5. Clofarabine
6. Nelarabine

DR ANKIT KUMAR (MEDED)


HGPRTase
1. 6 Thioguanine purine
fake

Hypoxanthine NEUCLEOTIDE
2. 6 Mercaptopurine Guanine Phospho Ribosyl
Transferase.
✗ ✗ DNA

uses: ① Lymphoma Not effective in Lysch Nyhan syndrome

Immunosuprisine (deficiency of HGPRTas e)


2

Sle: BM supression

Hepatotoxic

DR ANKIT KUMAR (MEDED)


6 Mercaptopurine
♀ AZATHIOPRINE
active
prodrug

SE 0 BM supression
not an Anticancer DRUG.
② Hepatotoxic → monitor ALT
"only Immunosuprinue DRUG"
↳ DOC IBD (UC/(D)

↑ Toxicity
Allopurinol
Xanthine oxidase
Febuxostat
Degraded outside Cell
♀ AZP GMP

TPMT (THIO PURINE Methyl Transferase)


Inside cell

① DOSE of AZP GMP should be Reduced by 75% (100 → 25) if gwent Allopurinol !

GMP → CI Genetic Depancy/mutation in Tpm, enzyme@ ↑ Toxicity


♀ AZP
DR ANKIT KUMAR (MEDED)
NEET

HAIRY All Leukemia


• Cladribine → DOC

DOC HISTIOCYTOSIS
MOA: Inhibit Adenosine
Deaminase
NEET
CLL FCR Regimen) (SCID)
• Fludarabine → DOC

Sf: MARKED Immunosupression

of all.
opportunistic infection I

→ Resistant cases Pneumocystis jeroxec.li


• Pentostatin
0
Give Corrimoxazole Prophylaxis against Pneumocystis

DR ANKIT KUMAR (MEDED)


* Cappillary leak syndrome
i pedriatic ALL
• Clofarabine

IE: Guillain Barre syndrome.


• Nelarabine : T Cell lymphoma

DR ANKIT KUMAR (MEDED)


Plant products as Anticancer DRUGS.

Vinca Alkaloid
M
① • Microtubule inhibitors phase

TAXANES

CAMPTOTHECIA
② • Topoisomerase inhibitors 92-S phase

E PIPODOPHYLLOTOXIN

DR ANKIT KUMAR (MEDED)


Microtubule inhibitors
M phase specific
inhibit , Metaphase
spindle arrest→
(poison) , Spindle poison
Metaphase Arrest at "M" phase.

Plant: PERI winkle plant WESTERN YEIN TREE

Moa: Inhibit Polymerization of Microtubule Inhibit Depolymerization of microtubule

→ 31 overstabilization of spindle
inhibit spindle
formation move
* ☁

DR ANKIT KUMAR (MEDED)


Transport Common s/E

microtubules ① NEUROTOXICITY
max: Vincristine > taxane.
② SIADH

③ PARALYTIC Ileus.
Vinca Taxane

Glove stock Neuropathy


Foot DROP

DR ANKIT KUMAR (MEDED)


Vinca Alkaloids

→ All types of lymphoma

Vincristine Adr: V0 BM supresian (cannot enter Bone)

↳ Not used in. OSTEOSARCOMA

Vin blastine → cause BM suprasion

DR ANKIT KUMAR (MEDED)


Taxanes
Q
< Nanoparticles of
> SI Allergy, Short acting Albumin
PACLITAXEL Paclitaxel
(unne enacted

DOCETAXEL
NAB - Paclitaxel
CABAZITAXEL
Nanoparticle Albumin Bound

Adv: Less Allergy


Hormone Resistant Cancer
use l Longer Acting
* BREAST Cancer

* PROSTRATE Cancer

CARDIAC STENT
② PACLITAXEL → Coated on DRUG ELUTING STents
Kf
• PACLITAXEL
stent (COBALT metal Q
To prevent Restenoses
◦ SIROLIMUS
cell growth due to growth of cells.
◦ EVEROLIMUS.

Restenosis DR ANKIT KUMAR (MEDED)


Some other microtubule inhibitors
Drugs Action Use

Eribulin ⊖ Polymerization of MT BREAST Cancer

Ixabiplone ⊖ Depolymerization → Breast cancer

Estramustine Depoly" - + Estrogen → Prostrate cancer

Colchicine ⊖ Depolyn ① ACUTE Gout

② KARYO typing

DR ANKIT KUMAR (MEDED)


Topoisomerase inhibitors S → uncoiling

92 → Coil
↳ maintain Topography/Coiling of DNA

↳ 92 = S Phase specific

l Camptothecin 2 Epipodophyllotoxin
• Irinotecan • Etoposide

• Topotecan • Teniposide

inhibit Topoisomerase - 1 Inhibit Topoisomerase 2

Plant

inhibit Floroquinolones (Antimicrobial)


BACTERIA → Top-4

DR ANKIT KUMAR (MEDED)


IRINOTECAN
↳ active form is SN-38 → SEE Severe Diarrhea

# of irinate can Diarrhea QQ

# CRIGGLER NAZZAR
• Topotecan LOPERAMIDE
& =
GILBERT Syndrome

(Rinotecan is metabolized by UDP-GT)


• Irinotecan
Depart in Criggler/Gilbert

DR ANKIT KUMAR (MEDED)


Anti-tumor Antibiotics
↳ obtained from STREPTOMYCES. BACTERIA

1. Anthracyclines (-rubicin)

2. Mitoxantrone v.Imp

3. Bleomycin

4. Actinomycin D

5. Mitomycin

6. Streptozotocin
DR ANKIT KUMAR (MEDED)
Anthracyclines (-rubicin)
Acton 92=5
MOA: Topoisomerase-2 inhibitor →
• Doxorubicin
• Daunorubicin Use: All cancers especially BREAST Cancer
CAT Regiment
• Epirubicin - cyclophosphamide
• Idarubicin - ADRIANYU I
• Valrubicin TAXANE DOXORUBICIN

stone → RED Color DRUGS


- RUBICIN: RUBY

Most cardiotoxic: Doxorubicin


no
CARDIOTOXICITY Least i) : IDARUBIC.us
¾
Red
> Antidote: DEXRAZOXANE
Dilated cardiomyopathy

DR ANKIT KUMAR (MEDED)


Mitoxantrone Top-2 inhibitor

Adv: Less cardiotoxic than Anthracycline

Uses

Multiple sclerosis

AML

Prostrate cancer Bony metastasis

DR ANKIT KUMAR (MEDED)


.x-Imp
Q.
Oxidative DNA Damage at
• Bleomycin 92 phase

Peptide Antibiotic

Use: HODGKIN lymphoma (ABV D)

Testicular cancer (BEP: Bleomycin, ETO POSIDE, Docetaxel)

HYDROLASE enzyme
PI: Bleomycin is Degraded by
Deficient
QQ. QQ

Skin
Longs
Flagellate pigments
Bleomycer Toxicity : PULMONARY FIBROSIS
ICTHYOSIS

Raynaud's
DR ANKIT KUMAR (MEDED)
Pulmonary FIBROSIS Typed cells: ↑ surfactant

1 Alveolar Cells.
Bleomycin: Damage Type Pulmonary Edw

I 02
FIBROSIS

Alveolar Cell Type 1 cell


Amiodanne: Damage Type 2
(> 95g.

Alveoli

Diagnosis: DL- CO l

* Diffusion of kung: Carbon monoxide

CO
?

DR ANKIT KUMAR (MEDED)


0 FLAGELLATE Pigmentation

0
Feather

ICTHYOSIS
Alveoli
BLEOMYCIN

(ISH like skin)

Raynaud's.

DR ANKIT KUMAR (MEDED)


Actinomycin D (dactinomycin)
MOA: Inhibit DNA Transcription

DOC WILM'S Tumor of kidney

Use: Childhood Tumors


DOC Rhabdomy ◦ sarcoma.

¥ Radiation Recall syndrome


* Damage skin that was previously exposed to Radiotherapy

Chemotherapy
Radiothery

DR ANKIT KUMAR (MEDED)


y.IM#

Mitomycin MOA: Alkylating Agent

Bladder cancer: Intra vesical injection (Also BCG vaccine)

Anti-FIBROTIC action (Reduce FIBROSIS


2

Mitomycin → Prevent Laryngo Tracheal stenosis after Radiotherapy

Bladder cancer
o
Radiothpy
SE: HUS-TTP an
INTRA VESICAL Cancer
} ing. 00.
↳ FIBROSIS (stenosis) ① MITOMYCIN
② BCG vaccine
larynx '↑ ↑ immunity (macrophage)
stimulant kill cancer
DR ANKIT KUMAR (MEDED)
I DIAZOXIDE
• Streptozotocin : Alkylating Agent
Reduce insulin sec"
OCTREOTIDE

DOC Insulinoma

kill β Cells: STREPTOZOTON

: Kills OSTEOCLAST
• Plicamycin (mithramycin) DOC

* was used for OSTEOPOROSIS BISPHOSPHONATES

PAGET's Disease

DR ANKIT KUMAR (MEDED)


Miscellaneous anti-cancer
AML-Type 3
(ACUTE PRO MY Elocytic Leukemia
1. Drugs for APML

÷ All TRANS RETINOIC ACID IRETINOIN


ATRA DOC

Resistant

Do not kill cancer cells


Arsenic trioxide MOA:

RAPID maturation of Cells


•a Rather:
v.v.Imp

Induce DIFFERENTIATION spontaneous Apotosis.

DR ANKIT KUMAR (MEDED)


ATRA
(Obesity, Diabetes, Dysupidonia)
IE . Metabolic syndrome

Lung DAMAGE
• Retinoic and syndrome →

* Rapid maturation of ⊛ cells in Lungs

Lung Damage.
Killed by WBC (inflammation)

I Dexamethasone before/after starting ATRA

DR ANKIT KUMAR (MEDED)


MEES
Lines
< Lung Damage

Retinoic acid syndrome by ATRA

I/+ Dexamethasone MEES Line (white lines a)


NAILS
Arsenic Trioxide

QT prolongation

DR ANKIT KUMAR (MEDED)


• L-Asparaginase > Enzyme from E. Coli

ALL → VPAD regimes


TI: ALL ≈

MOA: Degrade Asparagine in Lymphocyte

proteins: Clotting factors → ↑ Bleeding


* : Degrades
Albumin reduced *↓

Pancreatitis

DR ANKIT KUMAR (MEDED)


SUMMARY TIME

DR ANKIT KUMAR (MEDED)


SIADH: VINCRISTINE
Cerebellar toxicity : Cytosine Arabinoside
Ototoxicity: CISPLATIN GE
Most emetogenic: CISPLATIN
cyclophosphamide

Pulmonary fibrosis: BLEOMYCIN

Cardiotoxicity: DOXORUBICIN (Antidote:


VOD of liver: DEXRA2oXam)
Ve(nHoe❤ptahtiisctlveein fibr'?""""""
sus) (DEFIBROTIDES
Nephrotoxicity: CISPLATIN (Antidote: Imitosting

Hand foot syndrome: Hemorrhagic cystitis:


• 5FU Cyclophosphamide (Antidote: MESNAY
. CAPECIDABINE IFOSFAMide

Flagellate pigmentation: BLEOMYAS

Glove stock neuropathy: TAXANE

Chemo-Man Foot drop neuropathy: VINCRISTINE

DR ANKIT KUMAR (MEDED)


SUMMARY OF Cancer Regimens

DR ANKIT KUMAR (MEDED)


ABVD > > MOPP
HODGKINS LYMPHOMA ADRIAMYCIN MECHLORETHAMINE

1
BLEOMYCIN
VINBASTINE
ONCOVIN (VINCRISTINE)
PROCARBAZINE
Regimens of choice
FCR
CLL FLUDARABINE
DACARBAZINE PREDNISOLONE
3 CYCLOPHOSPHAMIDE
RITUXIMAB
CLADRIBINE HISTIOCYTOSIS, HAIRY CELL LEUKEMIA
AML 4
VPAD
ALL
7C + 3D
VINCRISTINE 8
RETINOBLASTOMA
CYTARABINE + DAUNORUBICIN 5
PREDNISOLONE VEC Q
7- days 3 days.
ASPARAGINASE VINCRISTINE
DAUNORUBICIN ETOPOSIDE
v.up
CARBOPLATIN
NON HODGKINS LYMPHOMA
6 COLORECTAL CANCER
2 R-CHOP
FOLFOX/FOLFIRI + BEVACIZUMAB
FOLINIC ACID 7
APML
RITUXIMAB
5-FU
CYCLOPHOSPHAMIDE ATRA
HYDROXY DAUNORUBICIN OXALIPLATIN/IRINOTECAN
ARSENIC TRIOXIDE
ONCOVIN
PREDNISOLONE DR ANKIT KUMAR (MEDED)
Targeted therapy in Cancer

1. Small molecules 2. Monoclonal antibodies C- MAB)

• Molecular wt < 500 Dalton

injections
peptide
✓ ORAL

others
Tyrosine kinase inhibitor

(-NIB)

DR ANKIT KUMAR (MEDED)


1 Gain function ②
Mutation

Cancer

Cell mems

IRAS RAF/MER

: Cell Division
signally
3

P 13K AKT/MTOR

DR ANKIT KUMAR (MEDED)


Tyrosine kinase receptors
inhibitors
* ORAL DRUGS
• -tinib
suff
'×: - NIB

MC S/E: Dianne (GIT)

• P/K: oral RASHES (Skin)

• Metabolized by CYP3A4  drug interaction


• S/E: Diarrhea, skin rashes

DR ANKIT KUMAR (MEDED)


BCR-ABL TKI nhibitor

QQ
Ponatinib, Uses:
DRUG to be
Imatinib, → 1ˢᵗ TKI
DOC ML
made
N
Nilotinib, CML
Chronic myeloid Leukemia
D
Dasatinib,
Balluchi
Bosutinib
Mutation: BCR-ABL mutation

(Philadelphia)

DR ANKIT KUMAR (MEDED)


Binds & inhibit ABL kinase

Tft CML

Imatinib 
Resistance to TKIs DOC: Dasatinib,
Nilotinib, Imatinib
Bosutinib 
Ponatinib
Resistant
→ Point mutation in ABL kinase

NILOTINIB, DASATIN/B, BOSUTINIB

Resistance

PONATINIB

DR ANKIT KUMAR (MEDED)


< Ttt: LOPERAMIDE
Imatinib me Sle : Diarrhea

• Dasatinib: pulmonary hypertension


* Pulmonary Hypertension &andPleural
pleural effusion
effusion

• Nilotinib and dasatinib: QT


* prolongation
QT prolongation

• Ponatinib: Arterial
Hepatotoxic
thrombosis and hepatotoxicity

DR ANKIT KUMAR (MEDED)


← Type of Tyrosine kinase receptor
Platelet-Derived Growth Factor
Receptor (c-KIT)
GASTRO - intestinal stromal tomer
Mutation GIST
CML BCR-ABL
S
• Sunitinib Imatinib
GIST PDGFR.
QQ
• Imatinib
• Regorafenib ✓ R RCC OVEGER.

sunitinib
☐ PDGFR
GIST

DR ANKIT KUMAR (MEDED)


Brutons tyrosine kinase inhibitor:

Lymphocyte

• Ibrutinib - BRUT
o

• Acalabrutinib Brutons
tyrosine
• Zanubrutinib kinase

MANTLE CELL LYMPHOMA


MARGINAL CELL LYMPHOMA lymphomas

CLL
SLL

DR ANKIT KUMAR (MEDED)


Non-small cell lung cancer
EGFR (HER1) INHIBITORS: ALK INHIBITORS:
(Anaplastic lymphoma kinase)
• ERLOTINIBEpidermal
(also Pancreatic Growth factor
cancer): food increasesReceptor
toxicity (HER-1) Crizotinib,
19
• GEFTINIB : no effect with food 2nd
2nd
①genER LOT IN IB ✓ → not given c- food: ↑ Absorption → ↑ toxicity
Alectinib,
CRIZOTINIB
• AFATINIB inhibitor of EGFR (HER1) and HER2
•② GEFTINIB
Dacomitinib
Brigatinib
BREGATINIB(first line agent now)
3rd gen QQ ① EGFR Ceritinib,
CERITINIB
•③OSIMERTINIB
AFATINIB 3rd
• Resistance to 1st and 2nd gen : T790M point mutation in TK: Osimertinib active in
this mutation
lorlatinib
④ OSIMERTINIB: Resistant cases
4th gen
(Due to point mutation: 7790 M) Q
• Mobocertinib : effective in all resistant cases

I → #NSCLC
• MAB approved: cetuximab, panitumumab, necitumumab
Antibody against EGFR DR ANKIT KUMAR (MEDED)
Human Epidermal Growth Factor Receptor 2
(HER2/Neu)

Mutation: Breast cancer


QQ
HER 2 new inhibitor LAPATINIB → #Trastuzumab resistant
• LAPATINIB
HER 2 + breast cancer
• Neratinib (inhibit both HER1 and HER2):
◦ NERATINIB
0
• Tucatinib: selective HER-2 inhibitor
• TUCATINIB.

• Use: HER2-positive trastuzumab-refractory breast cancer.

HER-1 → KI EGFR : causes lung cancer

Human Epidermal growth factor Receptor (HER)


-

BREAST Cancer
HER 2 DR ANKIT KUMAR (MEDED)
VEGFR: inhibit angiogenesis
VASC- endothelial growth factor receptor: formation of Blood vessels

Renal Cell Carcinoma : OVEGER Medullary Carcinoma Thyroid OVEGER


Q
P PAZOPANIB ☆☆
• VANDETANIB Vande → Mataram
t.JP Vanditanes Medullary 6
A AXITINIB • CABOZANITINIB
thyroid
SORAFENIB
S

S
SUNITINIB
S/E : Hypertension
Rate: Regorafenib
=
Low: Lenvatinib AML with FLT-3 mutation ◦ VEGER.

RCC • MIDOSTAURIN
sunttinus GIST • GILTERITINIB
VEGF –inhibition; Inhibitors of Tumor Angiogenesis
a
s/e: Hypertension,
sorafers → RCCthrombosis and bleeding
Hepatocellular Cancer

DR ANKIT KUMAR (MEDED)


KINASE SIGNALLING PATHWAY

→ MC : BRAF mutation

RAS Inhibitors MALIGNANT MELANOMA


QQ

NSCLC : Lung cancer a 1. BRAF INHIBITORS: RAF

kRAS Mutant Vemuraf enib, Dabrafenib, Encorafenib

2nd me mutation
• Sotorasib RAS 2. MEK INHIBITORS:
Adagrasib Tremet inib, Cobemet inib,

DR ANKIT KUMAR (MEDED)


Hyperglycemia
Metabolic syndrome

Inositol phosphate
kinase.
mTOR inhibitors Mammalian target

PI3K INHIBITOR of Rapamycin

Idelalisib LisiB
Sirolimus
Limus
Copanlisib Temsirolimus
Duvelisib Everolimus
Umbralisib DRUG eluting

Alpelisib cardiac stents

a
B CELL LYMPHOMA RCC, Breast cancer, PNET
(CLL, SLL, FL)
DR ANKIT KUMAR (MEDED)
CDK 4, 6 inhibitors - CICLIB Riociclib y.INT
= Abemaciclib
cyclin dependant kinase
a
Cell cycle transition
Palbociclib
ER + Breast cancer

G1 s Cell Arrest at G1 phase

Q
PARP inhibitors - PARIB Rucaparib
Iniparib
(Poly ADP Ribose Olaparib BRCA(+) Breast cancer
Phosphate) Talazoparib BRCA(+) Ovarian cancer

DR ANKIT KUMAR (MEDED)


EP/Genetic Action @

1 Vorinostat Cutaneous T cell Carcinoma


Histone Deacetylase
- NOSTAT Peripheral T cell Lymphoma
inhibitors Belinostat
methyl a
÷
Acetyl istone Panobinostat Multiple Myeloma

DNA → modify (EPIGENET;)

- Metostat epithelioid sarcoma


Histone Tazemetostat
Methyltransferase ✗ ✗
Inhibitors

DR ANKIT KUMAR (MEDED)


QQ

Proteosome inhibitor - ZOMIB Bortezomib Multiple myeloma

v.v.Imp
Carfilzomib DOC

Ixazomib
# Bortozoms
Mcd Along with dexa and
+
thalidomide
Thalidomide/Lenaledomide
+
Dexamethasone

Nuclear Export Inhibitor -INEXOR Selinexor Multiple myeloma


(inhibit XPO 1)
DLBCL
need

DR ANKIT KUMAR (MEDED)


Sonic hedgehog pathway - DEGIB Sonidegib Basal cell carcinoma
Inhibitor Vismodegib
(SMO)

AML
need Glasdegib

BCL-2 inhibitors - CLAX Venetoclax CLL with 17p deletion


Obatoclax
new

DR ANKIT KUMAR (MEDED)


Belzutifan  VHL cancers
MOA

Hypoxia inducible factor


• inhibitor of HIF-2α

• RCC (clear cell type), CNS hemangioblastomas, or


pancreatic NET. ☑ cancers in VHL

• S/E: Anaemia due to the reduction of erythropoietin


production
HIF

DR ANKIT KUMAR (MEDED)


Bcr-Abl Dasatinib, Non-small cell lung
TKI: Uses:
Bosutinib
Ponatinib, • CML
cancer EGFR INHIBITORS:
SORAFENIB • ERLOTINIB (also Pancreatic
Imatinib,
cancer)
Nilotinib, LENVATINIB
Summary • GEFTINIB
• OSIMERTINIB ← a
Sunitinib • AFATINIB
GIST HCC
Imatinib
then
Regorafenib ALK INHIBITORS:
Rember CRIZOTINIB, CERITINIB, ALECTINIB
Renal Cell Carcinoma (VEGRF
LAPATINIB BREAST CANCER inhibitors)
NERATINIB HER/Neu + • PAZOPANIB,
• AXITINIB J

VANDETANIB ✓
MEDULLARY CARCINOMA • SORAFENIB
CABOZANTINIB THYROID

DR ANKIT KUMAR (MEDED) SUNITINIB
MONOCLONAL ANTIBODIES
synthesized by
Antigen Antibody

g
66
Hybridoma Antibody

technique against
one Antigen
QQ

MAB

DR ANKIT KUMAR (MEDED)


Nomenclature TOSITO MO MAB -MO-

RITU ✗ i MAB -X1-

• Suffix: -mab
-RASTU ZU MAB -20-

• Source: - PANITU MU
MAB -MU-

• -mo mab (MOUSE),: mouse 100%


xi mab (CHIMERIC) 50% mouse & 50% human (MIXTURE)
• -a-
• -zu mab (HUMANIZED) > 95% human
mu mab (FULLY HUMAN) 100% human
• -If
Q ADALI MU MAB Fully Human

DR ANKIT KUMAR (MEDED)


MAB in tumors

Find "the" word

DR ANKIT KUMAR (MEDED)


Blocks
DOC
HER2/neu
.4.IM' TRASTUZUMAB HER2/neu + Breast cancer
(Erb-1)
Sf: CARDIO TOXIC

o
PERTUZUMAB
↑ RISK of cardio toxicity by
MAB
DOXORUBICIN

Link

MM Toxin: Kill cancer

Breast cancer
ADO-TRASTUZUMAB emtansine linked to DM1
(Microtubule cleaver)
TOXIN
v.v.Imp

Cetuximab Blocks
Q
1. ColoRectal cancer,
EGFR Q.
2. Head and neck cancer
(Erb-2)
(HER-1 Q
3. Non-Small Cell Lung Cancer
:
Panitumumab
Necitumumab
MAB ✗ " 10hTyrosine Kinase Receptor ⊕

NIB Cancer Divide


v.vamp
Rituximab
Blocks Re: Rheumatoid Arthritis° Re
a
L: Lupus erythematous (SLE) I: ITP L
CD20 (refractory) I
on A: AIHA
N: NHL (R-CHOP) A
B- lymphocyte
Ce: CLL
- (FCR) N

Ce
Obinutuzumab
new: Afutuzumab
ITP: idiopathic thrombocytopenic purpura
T.
Ofatumumab
AIHA: Autoimmune Hemolytic Ancence

NHL: non-Hodgken
CLL: chronic Lymphog we take.
DARATUMUMAB CD-38 MULTIPLE MYELOMA

ISATUXIMAB

ELOTUZUMAB CD 319 MULTIPLE MYELOMA

ALEMTUZUMAB CD52 Chronic lymphocytic leukemia


(2nd line to fludarabine)

DINUTUXIMAB GD2 Neuroblastoma in children


Immune Check Point Inhibitors
V.V.Imp
do

137/BS CTLAY
CTLAY
PD-I
I kill
supron
lymphocyte
lymphocyte Cancer cells Negative stimulus
> D- 1
PD-1 (immunity) Supress Lymphocyte

Q
Ipilimumab Nivolumab Q
Tremelimumab Atezolizumab Cepilimumab
Avelumab Pembrolizumab Q
C A4
Durvalumab
B%K²PD-1
Block CTLAY Block PPD'-1
( n n Ligand)
(Programme Death receptor)

DR ANKIT KUMAR (MEDED)


Immune Check Point Inhibitors
v. Vamp

Also Hodgkendyphone
New Nivolumab & Non small cell Lung Ca, Melanoma

Tumor Tremelimumab : 7) 1)

Drugs Durvalumab → endometrial Cancer

Acting Avelumab urothellal cancer y.x.JP

At Atezolizumab for
welcome
Immune Ipilimumab Q non small cell duy 6, /NICE exam

Check Cepilimumab " "


Q
Point Pembrolizumab : > 30 cancers
Pembrolizumab
Block PD-1

Pulmonary cancer
Large B cell lymphime.
(Lung cancer) melanomal Renal
ECG
Oesophagus
Endometrial Cancer stomach

Breast cancer Colorectal

(all GIT)

Pembroksumab in Lung cancer


◦ KEYNOTE TRIAL : Trial of

(INICET: 20233

DR ANKIT KUMAR (MEDED)


Immune check point inhibitors
1. Malignant Melanoma
IPILIMUMAB CTLA4 2. Non-Small cell lung cancer
TREMELIMUMAB

Summa
ATEZOLIMUMA B * 1. UROTHELIAL CANCER
AVELUMAB PD-L-1 2. ANAPLASTIC THYROID CANCER
(Programme death 3. Non-Small cell lung cancer
ligand)

DURVALUMAB Endometrial cancer (also Pembrolizumab)

NIVOLUMAB PD-1 receptor 1. Malignant Melanoma


PEMB ROLIZUMAB (Programme death) 2. Non Small cell lung cancer
3. Hodgkins lymphoma
Monoclonal antibody in Psoriasis References
Mcd
Block
a Ixekizumab
Secu kin u mab Brodalumab IL-17 Plaque Psoriasis

Tildrakizumab IL-23 Plaque Psoriasis

Guselkumab

Plaque Psoriasis
Ustekinumab IL-12 AND IL-23 &
IBD (UC/CD)

CD11a Plaque Psoriasis


Efalizumab

CD2 (LFA) Plaque Psoriasis


Alefacept
leewytee function Anger
MAB in SLE Blocks

BELIMUMAB BAFF SLE


(B CELL ACTIVATING
FACTOR)

MAB in type 1 diabetes mellitus


TEPLIZUMAB CD-3 TYPE 1 DM

MAB in Alzheimer's disease Blocks

ADUCANUMAB Q BETA 1 AMYLOID ALZHEIMERS DISEASE

LECANEMAB
AI
MAB FOR Paroxysmal nocturnal Hemoglobinuria MCG only

PNH
uses
Blocks
ECULIZUMAB C5 Complement Paroxysmal nocturnal Hemoglobinuria

RAVULIZUMAB HUS-TTP

PEGCETACOPLAN C5 Complement Paroxysmal nocturnal Hemoglobinuria


v.IN
MAB against Microbes Mcd only

✗ if so
PALIVIZUMAB Virus RSV Virus

QQ
BEZLOTOXUMAB Toxin B of Psuedomembranous Colitis
Clostridium difficile
QQ
RAXIBACUMAB Bacteria Anthrax

OBILTOXAXIMAB
ANGIOGENESIS inhibit VEGER
VASC. endothelial growth factor
INHIBITORS
DRUGS TARGET USE
QQ

BEVACIZUMAB ✗ up → VEGF
COLORECTAL CANCER

RAMUCIRUMAB VEGFR
Truptor
Q
BEVACIZUMAB
RA NIBIZUMAB Diabetic RETINOPATHY
Intravitreal inj.
ALFIBERCEPT In eye ARMD-WET TYPE
↓ (Age Related macular degenem)
PEGAPTANIB
0 Neovascularization on Rehne

DR ANKIT KUMAR (MEDED)


MAB

Q
Armed Monoclonal antibodies no Toxin liak

BRENTUXIMAB VEDONTIN CD30 + Vedontin Hodgkin’s Lymphoma


(Microtubule cleaver) large cell lymphoma
GEMTUZUMAB QQ CD 33+ Calicheamicin Relapsed AML
OZOGAMICIN
(Toxin)

Moxetumomab pasudotox CD 22 Hairy cell leukemia


Linked to psuedomonas
toxin A

Resistant cancer
Mcdonly

DR ANKIT KUMAR (MEDED)


Mcd only
ytterium" iodine""

Y90 IRBITUMOMAB CD 20 + Radioisotope Relapsed Non-Hodgkin’s


a
Lymphoma
I131 TOSITUMOMAB
DENILEUKIN DIFITOX IL-2 Cutaneous T cell lymphomas
(IMMNUNOTOXIN) linked with Diphtheria
toxin

DR ANKIT KUMAR (MEDED)


Q Q

Immunosuppression DRUG thalidomide

Pharma Friday PIN-MEDED

DR ANKIT KUMAR (MEDED)


dr-ankit"

Ankit"

Wishes
hanks & Best
n n

and
¥ Dehydration → vomiting/ Dianne
DKA

Hyperglycemic Hyperoshler
state
✓ typet ketones HARRISON: Read

Type 2
1ˢᵗ 7ft: HYDRATIM → ⑪ saline

shift to skinsuler
insulin (till Blood glucose < 200)
in Regular
ketones are negative

* Treat infections
Sodium Bicarbonate
KU 1 if + +

kt supplement (¥ Metabolic acidosis)

DR ANKIT KUMAR (MEDED)

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