Table 1.

Classes of GPCR-Targeted Drugs Discussed in This Review

Class	Medication	Primary indications	Primary GPCR target	Number of cancer-related PubMed search results (August 2020)	Mostly antitumorigenic (+), or both pro- and antitumorigenic (+/−)
Cardiac	β-Blockers	Hypertension, arrhythmia, anxiety, migraine headaches	β-Adrenergic receptors	334	+
	Vorapaxar	Thrombosis, history of myocardial infarction or peripheral arterial disease	Protease-activated receptor 1 (PAR1)	15	+
	Clopidogrel	Risk of myocardial infarction or stroke	P2Y12	241	+
	Aspirin	Chemoprevention, fever, arthritis, risk of myocardial infarction or stroke	Prostanoid receptors	4375	+
Antiemetic/analgesic	Neurokinin-1 receptor antagonists	Nausea, vomiting	Neurokinin 1 (NK-1R) receptors	131	+
	Dronabinol/THC	Nausea, vomiting, anorexia, appetite stimulant	GPR55, cannabinoid receptors 1 and 2 (CB1/CB2)	344/361	+/−
	Cannabinoids	Anxiety, nausea, appetite stimulant	GPR55, cannabinoid receptors 1 and 2 (CB1/CB2)	1009	+/−
	Opioids	Moderate to severe pain	μ, δ, and κ opioid receptors	8286	+/−
Anti-Inflammatory	Leukotriene receptor antagonists (LTRAs)	Asthma, allergies	Cysteinyl leukotriene receptors	12	+
	Antihistamines	Allergies, cold and flu symptoms, motion sickness Acid reflux, stomach ulcers	Histamine H1 receptor (HRH1) HRH2	152	+/−
Antidiabetic	Glucagon-like peptide 1 agonists	Type II diabetes mellitus	Glucagon-like peptide 1 (GLP-1) receptors	20	+/−
Parasympathetic	Muscarinic/cholinergic agonist/antagonists	Glaucoma, bladder/gastrointestinal disorders, chronic obstructive pulmonary disease	Cholinergic receptor muscarinic 1–5 (CHRM 1–5)	27/31	+/−
Neuropsychiatric	Selective serotonin reuptake inhibitors (SSRIs)	Depression, anxiety, post-traumatic stress disorder, obsessive compulsive disorder	5-Hydroxytryptamine (5-HT) receptors	110	+/−
	Antiemetic dopamine antagonists	Nausea, schizophrenia, bipolar disorder	Dopamine receptors 1–5 (D1R–D5R)	9	+/−