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Oncology

Targeted Chemo Therapies

Drug	Pharmacologic Class	Molecular Target(s)	Gene(s)	Normal Role of Target	Cancer Pathophysiology	Mechanism of Action	Key Adverse Effects / Warnings	Resistance / Clinical Pearls
Gefitinib	EGFR TKI	EGFR	EGFR	Growth factor signaling	Activating EGFR mutations cause uncontrolled proliferation	Reversible inhibition of EGFR tyrosine kinase	Rash, diarrhea, ILD	High primary resistance; T790M secondary resistance
Lapatinib	EGFR/HER2 TKI	EGFR, HER2	EGFR, ERBB2	Cell growth and differentiation	HER2 overexpression drives signaling	Reversible dual EGFR/HER2 inhibition	Hepatotoxicity (BBW)	Avoid grapefruit; CYP3A4 metabolism
Tucatinib	HER2 TKI	HER2	ERBB2	Cell growth signaling	HER2 amplification	Highly selective HER2 inhibition	Diarrhea, hepatotoxicity	Minimal EGFR inhibition → fewer skin AEs
Afatinib	EGFR/HER2/HER4 TKI	EGFR, HER2, HER4	EGFR, ERBB2	Growth signaling	Constitutive ErbB signaling	Irreversible ErbB family inhibition		Less resistance than first‑gen EGFR TKIs
Osimertinib	EGFR TKI	EGFR variants	EGFR	Growth signaling	T790M & activating mutations	Irreversible mutant‑selective EGFR inhibition	ILD, pneumonitis, PE	Designed for T790M resistance
Cetuximab	mAb	EGFR	EGFR	Cell proliferation	EGFR overexpression	Blocks ligand binding + ADCC	Infusion reactions (BBW), rash	KRAS must be wild‑type
Panitumumab	mAb	EGFR	EGFR	Cell proliferation	EGFR overexpression	Fully human EGFR blockade	Dermatologic toxicity (BBW)	KRAS testing required
Trastuzumab	mAb	HER2	ERBB2	Growth signaling	HER2 overexpression	Blocks HER2 + ADCC	Cardiomyopathy (BBW)	Avoid anthracyclines
Ado‑trastuzumab emtansine	ADC	HER2	ERBB2	Growth signaling	HER2 overexpression	HER2‑directed delivery of DM1	Hepatotoxicity, cardiotoxicity	Do not substitute for trastuzumab
Fam‑trastuzumab deruxtecan	ADC	HER2	ERBB2	Growth signaling	HER2 overexpression	HER2‑directed topoisomerase I inhibitor	ILD/pneumonitis (BBW)	High potency; bystander effect
Pertuzumab	mAb	HER2	ERBB2	Receptor dimerization	HER2 signaling amplification	Prevents HER2 dimerization	LV dysfunction	Synergistic with trastuzumab
Crizotinib	ALK TKI	ALK, ROS1, MET	ALK	Neural development	ALK fusion proteins	Inhibits ALK phosphorylation	QT prolongation, ILD	Resistance common
Alectinib	ALK TKI	ALK, RET	ALK	Neural development	ALK fusion proteins	Second‑gen ALK inhibition	Bradycardia, hepatotoxicity	Good CNS penetration
Brigatinib	ALK TKI	ALK, ROS1, FLT3	ALK	Neural development	ALK fusion proteins	Second‑gen ALK inhibition	Pulmonary toxicity	Dose escalation required
Ensartinib	ALK TKI	ALK, ROS1, MET	ALK	Neural development	ALK fusion proteins	Second‑gen ALK inhibition	ILD, CNS toxicity	CYP3A4 metabolism
Lorlatinib	ALK TKI	ALK, ROS1	ALK	Neural development	ALK resistant mutations	Third‑gen ALK inhibition	Hepatotoxicity	Active vs resistant ALK mutations
Midostaurin	FLT3 TKI	FLT3	FLT3	Hematopoiesis	FLT3 ITD/TKD mutations	FLT3 inhibition → apoptosis	Pulmonary toxicity	Used with chemotherapy
Quizartinib	FLT3 TKI	FLT3	FLT3	Hematopoiesis	FLT3 ITD mutations	Potent FLT3 inhibition	QT prolongation (BBW)	Contraindicated in long QT
Larotrectinib	TRK TKI	TRKA/B/C	NTRK1‑3	Neural development	NTRK gene fusions	Selective TRK inhibition	Neurotoxicity	Tumor‑agnostic
Entrectinib	TRK TKI	TRK, ROS1, ALK	NTRK1‑3	Neural development	NTRK fusions	Multi‑kinase TRK inhibition	CHF, QT prolongation	Crosses BBB
Repotrectinib	TRK TKI	TRK, ROS1	NTRK1‑3	Neural development	TRK resistance mutations	Second‑gen TRK inhibition	Neurotoxicity	Active vs TRK variants
Selpercatinib	RET TKI	RET	RET	Organ development	RET fusions/mutations	Selective RET inhibition	Hepatotoxicity, HTN	QTc monitoring
Pralsetinib	RET TKI	RET	RET	Organ development	RET mutations	Selective RET inhibition	ILD, HTN	CYP3A metabolism
Capmatinib	MET TKI	MET	MET	Cell migration	MET exon 14 skipping	Selective MET inhibition	Peripheral edema	Exon 14 specific
Tepotinib	MET TKI	MET	MET	Cell migration	MET exon 14 skipping	Selective MET inhibition	Edema, fatigue	Similar to capmatinib
Amivantamab	Bispecific mAb	EGFR, MET	EGFR, MET	Growth signaling	EGFR exon 20 insertions	EGFR/MET blockade + ADCC	Infusion reactions	For exon 20 disease
Acalabrutinib	BTK inhibitor	BTK	BTK	B‑cell signaling	B‑cell malignancies	Irreversible BTK inhibition	Bleeding	Less CV toxicity than ibrutinib
Zanubrutinib	BTK inhibitor	BTK	BTK	B‑cell signaling	B‑cell malignancies	Irreversible BTK inhibition	Myelosuppression	More selective BTK
Palbociclib	CDK4/6 inhibitor	CDK4/6	CDK4, CDK6	Cell cycle progression	Uncontrolled G1→S transition	Cell cycle arrest	Neutropenia	CYP3A interactions
Ribociclib	CDK4/6 inhibitor	CDK4/6	CDK4, CDK6	Cell cycle progression	Uncontrolled proliferation	Cell cycle arrest	QT prolongation	ECG monitoring
Bevacizumab	Angiogenesis inhibitor	VEGF‑A	VEGFA	Angiogenesis	Tumor neovascularization	Neutralizes VEGF	Bleeding, HTN	Impaired wound healing
Atezolizumab	ICI	PD‑L1	CD274	Immune tolerance	Immune evasion	Blocks PD‑L1	Autoimmune AEs	Tumor‑expressed ligand
Durvalumab	ICI	PD‑L1	CD274	Immune tolerance	Immune evasion	Blocks PD‑L1	Immune AEs	Used post‑chemoradiation
Nivolumab	ICI	PD‑1	PDCD1	Immune tolerance	Immune evasion	Blocks PD‑1	Immune AEs	Broad tumor use
Pembrolizumab	ICI	PD‑1	PDCD1	Immune tolerance	Immune evasion	Blocks PD‑1	Immune AEs	PD‑L1 guided use
Cemiplimab	ICI	PD‑1	PDCD1	Immune tolerance	Immune evasion	Blocks PD‑1	Immune AEs	Cutaneous SCC
Blinatumomab	BiTE	CD19/CD3	CD19	B‑cell signaling	B‑cell leukemia	T‑cell redirected cytotoxicity	Cytokine release syndrome	Continuous infusion
Rituximab	mAb	CD20	MS4A1	B‑cell marker	B‑cell malignancy	CD20‑directed ADCC	Infusion reactions	HBV reactivation
Obinutuzumab	mAb	CD20	MS4A1	B‑cell marker	B‑cell malignancy	Enhanced ADCC	Infusion reactions	More potent than rituximab
Venetoclax	BCL‑2 inhibitor	BCL‑2	BCL2	Prevents apoptosis	Cancer cell survival	Restores apoptosis	Tumor lysis syndrome	Ramp‑up dosing
Asparaginase	Enzyme	Asparagine	ASNS	Protein synthesis	Leukemic cells lack asparagine synthesis	Depletes asparagine	Pancreatitis, thrombosis	Hypersensitivity common
Asparaginase erwinia	Enzyme	Asparagine	ASNS	Protein synthesis	Leukemic dependence	Asparagine depletion	Hypersensitivity	Used if E. coli allergy

Created by: CaristW

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