Dataset S1: Drugs from the top-100 best-selling drugs list that target circadian genes. |
|
|
|
|
|
|
|
|
Rank |
Sales |
Trade name |
Drug |
Indications |
Circadian-gene targets |
Organs in which targets oscillate |
1 |
$1.53 b |
Abilify |
aripiprazole |
Bipolar disorder, Major depressive disor... |
Htr2c, Htr1b, Htr2a, Chrm2, Drd4, Adra2b, Adra1b, Adra1a |
lung, heart, brainstem, white fat, adrenal gland, liver, brown fat, kidney, skeletal muscle, cerebellum |
2 |
$1.46 b |
Nexium |
esomeprazole |
Gastritis, GERD, Esophagitis |
Atp4a |
liver |
3 |
$1.30 b |
Cymbalta |
duloxetine |
Chronic pain, Fibromyalgia, Diabetic neu... |
Slc6a4 |
adrenal gland, kidney |
4 |
$1.30 b |
Crestor |
rosuvastatin |
Hyperlipidemia |
Hmgcr, Abcc1, Abcc4 |
lung, heart, hypothalamus, liver, brown fat |
5 |
$1.28 b |
Advair Diskus |
fluticasone + salmeterol |
Asthma, Chronic obstructive pulmonary di... |
Serpina6, Pgr, Nr3c2, Adrb2, Pla2g4a |
lung, heart, liver, kidney, skeletal muscle, aorta |
6 |
$1.22 b |
Humira |
adalimumab |
Rheumatoid arthritis, Crohn's disease, U... |
Fcgr2b, Fcgr3 |
liver, kidney |
7 |
$1.08 b |
Enbrel |
etanercept |
Rheumatoid arthritis, Psoriasis |
Fcgr2b, Tnfrsf1b, Fcgr3 |
hypothalamus, liver, kidney |
10 |
$859 m |
Neulasta |
filgrastim |
Acute myeloid leukemia |
Csf3r |
lung |
11 |
$794 m |
Rituxan |
rituximab |
Rheumatoid arthritis, Non-Hodgkin's lymp... |
Fcgr2b, Ms4a1, Fcgr3 |
liver, kidney, skeletal muscle |
12 |
$726 m |
Spiriva |
tiotropium |
Chronic obstructive pulmonary disorder |
Slc22a5, Slc22a4, Chrm2 |
heart, brainstem, brown fat, kidney, aorta |
14 |
$701 m |
Januvia |
sitagliptin |
Diabetes mellitus T2 |
Abcb1a, Dpp4 |
heart, adrenal gland, liver, kidney |
16 |
$641 m |
Avastin |
bevacizumab |
Colorectal cancer, Non-small cell lung c... |
Fcgr2b, Vegfa, Fcgr3 |
heart, brown fat, liver, kidney, skeletal muscle, aorta |
17 |
$637 m |
Lantus Solostar |
insulin glargine |
Diabetes mellitus T2 |
Igf1r |
kidney |
18 |
$592 m |
Lantus |
insulin glargine |
Diabetes mellitus T2 |
Igf1r |
kidney |
20 |
$538 m |
Diovan |
valsartan + hydrochlorothiazide |
Hypertension, Heart failure |
Slc22a6, Agtr1a, Slco1b2, Car4, Kcnma1, Car12, Car2 |
heart, adrenal gland, liver, kidney, skeletal muscle |
22 |
$518 m |
Celebrex |
celecoxib |
Osteoarthritis, Rheumatoid arthritis |
Ptgs2, Pdpk1, Abcc4 |
lung, brainstem, brown fat, aorta, cerebellum |
24 |
$471 m |
Herceptin |
trastuzumab |
Breast cancer |
Fcgr2b, Erbb2, Egfr, Fcgr3 |
heart, liver, kidney |
26 |
$438 m |
Gleevec |
imatinib |
Chronic myeloid leukemia |
Ptgs1, Kit, Slc22a2, Abcg2, Pdgfra, Pdgfrb, Ddr1, Abca3, Abl1, Ret, Abcb1a |
lung, heart, brainstem, white fat, adrenal gland, brown fat, liver, kidney |
27 |
$431 m |
Vyvanse |
lisdexamfetamine |
Attention deficit hyperactivity disorder |
Adra1b |
liver |
29 |
$415 m |
Lucentis |
ranibizumab |
Macular degeneration |
Vegfa |
heart, brown fat, liver, skeletal muscle, aorta |
30 |
$413 m |
Synagis |
palivizumab |
Respiratory syncytial virus |
Fcgr2b, Fcgr3 |
liver, kidney |
31 |
$395 m |
Zetia |
ezetimibe |
Hyperlipidemia |
Soat1, Abcc2, Anpep, Abcb1a |
lung, heart, brainstem, adrenal gland, liver, kidney |
32 |
$392 m |
Tamiflu |
oseltamivir |
Influenza |
Neu2, Neu1, Ces1g, Slc22a8, Slc15a1, Abcc4 |
lung, liver, brown fat, kidney, cerebellum |
33 |
$383 m |
Ritalin |
methylphenidate |
Attention deficit hyperactivity disorder |
Slc6a4 |
adrenal gland, kidney |
34 |
$377 m |
Symbicort |
budesonide + formoterol |
Asthma, Chronic obstructive pulmonary di... |
Adrb2 |
lung, kidney, skeletal muscle |
36 |
$365 m |
Lovenox |
enoxaparin |
Deep vein thrombosis, Myocardial infarct... |
Serpinc1 |
liver |
37 |
$348 m |
AndroGel |
testosterone |
Hypogonadism |
Slc22a4, Slc22a3, Ar, Cyp1a1, Cyp2b10, Akr1d1, Abcg2, Cyp1b1, Cyp17a1, Cyp2a5, Slc22a8, Abcb1a, Maoa |
lung, heart, brainstem, white fat, adrenal gland, liver, brown fat, kidney, aorta, cerebellum |
38 |
$346 m |
Lidoderm |
lidocaine |
Pain |
Slc22a5, Cyp2b10, Egfr, Abcb1a |
lung, heart, adrenal gland, brown fat, liver, kidney, aorta |
39 |
$338 m |
Avonex |
interferon beta-1a |
Multiple sclerosis |
Ifnar2 |
skeletal muscle |
41 |
$332 m |
Rebif |
interferon beta-1a |
Multiple sclerosis |
Ifnar2 |
skeletal muscle |
44 |
$304 m |
Seroquel XR |
quetiapine |
Bipolar disorder, Major depressive disor... |
Htr2c, Htr1b, Htr2a, Chrm2, Drd4, Adra1d, Adra2b, Abcb1a, Adra1b, Adra1a |
lung, heart, brainstem, white fat, adrenal gland, brown fat, liver, kidney, skeletal muscle, cerebellum |
45 |
$289 m |
Viagra |
sildenafil |
Erectile dysfunction |
Cyp1a1, Pde6g, Abcc5, Abcc10, Pde5a, Cyp2e1, Abcc4 |
lung, heart, brainstem, white fat, adrenal gland, hypothalamus, brown fat, kidney, aorta, cerebellum |
47 |
$281 m |
Niaspan |
niacin |
Hyperlipidemia |
Slco2b1, Slc22a5, Qprt, Slc16a1 |
lung, heart, brainstem, adrenal gland, white fat, hypothalamus, liver, brown fat, kidney, aorta, cerebellum |
48 |
$279 m |
Humalog |
insulin lispro |
Diabetes mellitus T2 |
Igf1r |
kidney |
49 |
$274 m |
Alimta |
pemetrexed |
Mesothelioma, Non-small cell lung cancer |
Tyms, Atic, Gart, Slc29a1 |
lung, heart, brainstem, brown fat, liver, kidney, aorta |
51 |
$268 m |
Tricor |
fenofibrate |
Hyperlipidemia |
Ppara |
lung, heart, white fat, adrenal gland, brown fat, liver, kidney |
54 |
$267 m |
Combivent |
ipratropium bromide + salbutamol |
Asthma, Chronic obstructive pulmonary di... |
Slc22a5, Slc22a4, Chrm2, Adrb1, Adrb2 |
lung, heart, brainstem, brown fat, kidney, skeletal muscle, aorta |
56 |
$262 m |
ProAir HFA |
salbutamol |
Asthma, Chronic obstructive pulmonary di... |
Adrb1, Adrb2 |
lung, kidney, skeletal muscle |
57 |
$253 m |
Cialis |
tadalafil |
Erectile dysfunction |
Pde5a |
adrenal gland |
62 |
$240 m |
Janumet |
metformin + sitagliptin |
Diabetes mellitus T2 |
Slc47a1, Slc22a2, Prkab1, Abcb1a, Dpp4 |
heart, brainstem, adrenal gland, hypothalamus, liver, brown fat, kidney |
63 |
$240 m |
Neupogen |
filgrastim |
Acute myeloid leukemia |
Csf3r |
lung |
66 |
$236 m |
Toprol XL |
metoprolol |
Hypertension, Heart failure |
Slc22a2, Adrb1, Adrb2, Abcb1a |
lung, heart, adrenal gland, brown fat, liver, kidney, skeletal muscle |
70 |
$220 m |
VESIcare |
solifenacin |
Overactive bladder |
Chrm2 |
heart, brainstem |
71 |
$220 m |
Vytorin |
ezetimibe + simvastatin |
Hyperlipidemia |
Hmgcr, Cyp2b10, Soat1, Abcc2, Anpep, Abcb1a |
lung, heart, brainstem, adrenal gland, brown fat, liver, kidney, aorta |
73 |
$219 m |
Provigil |
modafinil |
Narcolepsy, Shiftwork sleep disorder |
Cyp2b10, Adra1b |
lung, brown fat, liver, aorta |
78 |
$209 m |
Aciphex |
rabeprazole |
Gastritis, GERD, Esophagitis |
Cyp1a1, Atp4a, Abcg2 |
lung, heart, brainstem, white fat, liver, brown fat, kidney |
83 |
$201 m |
Synthroid |
levothyroxine |
Hypothyroidism |
Slc16a2, Serpina7, Thrb, Thra, Abcb1a |
lung, heart, white fat, adrenal gland, brown fat, liver, kidney, aorta, skeletal muscle, cerebellum |
84 |
$198 m |
Evista |
raloxifene |
Osteoporosis |
Ncoa2, Cyp2b10, Esr1, Esr2 |
lung, white fat, brown fat, liver, kidney, aorta |
87 |
$196 m |
Betaseron |
interferon beta-1b |
Multiple sclerosis |
Ifnar2 |
skeletal muscle |
88 |
$193 m |
Lipitor |
atorvastatin |
Hyperlipidemia |
Hmgcr, Cyp2b10, Ahr, Abcc5, Abcc1, Abcb1a, Abcc4, Dpp4 |
lung, heart, brainstem, white fat, adrenal gland, hypothalamus, brown fat, liver, kidney, aorta, cerebellum |
90 |
$189 m |
Lunesta |
eszopiclone |
Insomnia |
Ptgs1, Tspo, Gabra3 |
lung, heart, adrenal gland, kidney |
97 |
$175 m |
Xeloda |
capecitabine |
Breast cancer, colorectal cancer |
Cda, Tymp, Tyms, Ces1g, Dpyd |
lung, adrenal gland, liver, brown fat, kidney, aorta |
98 |
$173 m |
Prilosec |
omeprazole |
Gastritis, GERD, Esophagitis |
Cyp1a1, Atp4a, Abcg2, Cyp1b1, Abcb1a |
lung, heart, brainstem, white fat, adrenal gland, brown fat, liver, kidney |
99 |
$171 m |
Focalin XR |
dexmethylphenidate |
Attention deficit hyperactivity disorder |
Slc6a4 |
adrenal gland, kidney |