Tasosartan

Tasosartan
Clinical data

Pregnancy category	N/A
ATC code	C09CA05 (WHO)
Legal status
Legal status	Withdrawn
Identifiers
IUPAC name 2,4-dimethyl-8-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one
CAS Number	145733-36-4^Y
PubChem (CID)	60919
IUPHAR/BPS	6898
DrugBank	DB01349^Y
ChemSpider	54890^N
UNII	48G92V856H^Y
Chemical and physical data
Formula	C₂₃H₂₁N₇O
Molar mass	411.459 g/mol
^NY (what is this?) (verify)

Tasosartan is an angiotensin II receptor antagonist.

It was withdrawn from FDA review by the manufacturer after phase III clinical trials showed elevated transaminases (a sign of possible liver toxicity) in a significant number of participants given the drug.^[1]^[2]

References

↑ Atkinson AJ, et al. (2007). Principles of clinical pharmacology. Amsterdam: Elsevier. p. 515. ISBN 0-12-369417-5.
↑ Dina R, Jafari M (July 2000). "Angiotensin II-receptor antagonists: an overview". Am J Health Syst Pharm. 57 (13): 1231–41. PMID 10902066.

Antihypertensives: agents acting on the renin–angiotensin system (C09)

ACE inhibitors ("-pril")	Sulfhydryl-containing: Captopril Rentiapril Zofenopril Dicarboxylate-containing: Enalapril^# Benazepril Cilazapril Delapril Imidapril Lisinopril (+HCT) Moexipril Perindopril (+indapamide) Quinapril (+HCT) Ramipril Spirapril Temocapril Trandolapril Phosphonate-containing: Fosinopril (+HCT) Other/ungrouped: Alacepril

AIIRAs ("-sartan")	Azilsartan Candesartan Eprosartan Fimasartan Irbesartan Losartan (+HCT) Olmesartan (+amlodipine) Tasosartan^§ Telmisartan (+HCT) Valsartan (+HCT, +amlodipine, +sacubitril)

Renin inhibitors ("-kiren")	Aliskiren (+amlodipine, +amlodipine and HCT) Remikiren^§

^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

Protein and peptide receptor modulators

Adiponectin

AdipoR₁	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon (–)-Arctigenin Arctiin Gramine Matairesinol Antagonists: Peptide: ADP-400

AdipoR₂	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon Deoxyschizandrin Parthenolide Syringing Taxifoliol Antagonists: Peptide: ADP-400

Angiotensin

Agonists: Angiotensin II
Angiotensin III
Angiotensin IV
Saralasin

Antagonists: Abitesartan
Azilsartan
Azilsartan medoxomil
Candesartan
Elisartan
Embusartan
Eprosartan
EXP-3174
Fimasartan
Forasartan
Irbesartan
Losartan
Milfasartan
Olmesartan
Olmesartan medoxomil
PD123319
Pomisartan
Pratosartan
Ripisartan
Saprisartan
Sparsentan
Tasosartan
Telmisartan
Valsartan
Zolasartan

Renin inhibitors: Aliskiren
Ciprokiren
Ditekiren
Enalkiren
Pepstatin
Remikiren
Terlakiren
Zankiren

Propeptides: Angiotensinogen
Angiotensin I

Bradykinin

Agonists: Bradykinin
Kallidin

Antagonists: FR-173657
Icatibant
LF22-0542

CGRP

Agonists: Amylin
CGRP
Pramlintide

Antagonists: BI 44370 TA
BMS-927711
CGRP (8-37)
MK-3207
Olcegepant
Rimegepant
SB-268262
Telcagepant
Ubrogepant

Antibodies: ALD403
Eptinezumab
Erenumab
Fremanezumab

Cholecystokinin

CCK_A	Agonists: Cholecystokinin Antagonists: Amiglumide Asperlicin Devazepide Dexloxiglumide Lintitript Lorglumide Loxiglumide Pranazepide Proglumide Tarazepide Tomoglumide

CCK_B	Agonists: Cholecystokinin CCK-4 Gastrin Pentagastrin (CCK-5) Antagonists: CI-988 (PD-134308) Itriglumide L-365,360 Netazepide Proglumide Spiroglumide

Unsorted	Antagonists: Nastorazepide

CRH

CRF₁	Agonists: Cortagine Corticorelin Corticotropin releasing hormone Sauvagine Stressin I Urocortin Antagonists: Antalarmin Astressin-B CP-154,526 Emicerfont Hypericin LWH-234 NBI-27914 Pexacerfont R-121919 TS-041 Verucerfont

CRF₂	Agonists: Corticorelin Corticotropin releasing hormone Sauvagine Urocortin Antagonists: Astressin-B

Cytokine

See here instead.

Endothelin

Agonists: Endothelin 1
Endothelin 2
Endothelin 3
IRL-1620

Antagonists: A-192621
ACT-132577
Ambrisentan
Atrasentan
Avosentan
Bosentan
BQ-123
BQ-788
Clazosentan
Darusentan
Edonentan
Enrasentan
Fandosentan
Feloprentan
Macitentan
Nebentan
Sitaxentan
Sparsentan
Tezosentan
Zibotentan

Galanin

GAL₁	Agonists: Galanin Galanin (1-15) Galanin-like peptide Galmic Galnon Antagonists: C7 Dithiepine-1,1,4,4-tetroxide Galantide (M15) M32 M35 M40 SCH-202596

GAL₂	Agonists: Galanin Galanin (1-15) Galanin (2-11) Galanin-like peptide Galmic Galnon J18 Antagonists: C7 Galantide (M15) M32 M35 M40 M871

GAL₃	Agonists: Galanin Galanin (1-15) Galmic Galnon Antagonists: C7 Galantide (M15) GalR3ant HT-2157 M32 M35 M40 SNAP-37889 SNAP-398299

Ghrelin/GHS

Agonists: Peptide: Alexamorelin
Cortistatin-14
Examorelin (hexarelin)
Ghrelin
GHRP-1
GHRP-3
GHRP-4
GHRP-5
GHRP-6
Ipamorelin
Lenomorelin
Pralmorelin (GHRP-2)
Relamorelin
Tabimorelin
Ulimorelin; Non-peptide: Adenosine
Anamorelin
Capromorelin
CP-464709
Ibutamoren (MK-677)
L-692,585
Macimorelin
SM-130686; Unsorted: LY-426410
LY-444711

Antagonists: A-778193
Cortistatin-8
(D-Lys³)-GHRP-6
JMV2959
YIL-781

Binding proteins: Growth hormone-binding protein

Agonists: Bovine somatotropin
Efpegsomatropin
Growth hormone
Human placental lactogen
Somagrebove
Somapacitan
Somatosalm
Somatotropin
Somatropin pegol
Somatrem
Sometribove
Somatrogon (MOD-4023; hGH-CTP)
Somavaratan
Somavubove
Somidobove

Antagonists: G120K-hGH
Pegvisomant

GHRH

Agonists: Peptide: CJC-1295
Dumorelin
GHRH
Modified GRF (1-29)
Rismorelin
Sermorelin
Somatorelin
Tesamorelin

Antagonists: MZ-5-156

GLP

GLP-1	Agonists: Albiglutide Dulaglutide Efpeglenatide Exenatide GLP-1 Langlenatide Liraglutide Lixisenatide Oxyntomodulin Semaglutide Taspoglutide

GLP-2	Agonists: Elsiglutide GLP-2 Teduglutide

Others	Propeptides: Preproglucagon Proglucagon

Glucagon

Agonists: Glucagon
Oxyntomodulin

Antagonists: Adomeglivant
L-168,049
LGD-6972

Propeptides: Preproglucagon
Proglucagon

GnRH

Antagonists: Peptide: Abarelix
Acyline
Cetrorelix
Degarelix
Detirelix
Ganirelix
Iturelix
Ozarelix
Prazarelix
Ramorelix
Teverelix (antarelix); Non-peptide: ASP-1707
Elagolix
KLH-2109
Relugolix
Sufugolix

Gonadotropin

LH/CG	Agonists: Choriogonadotropin alfa Human chorionic gonadotropin Luteinizing hormone Lutropin alfa Menotropin (human menopausal gonadotropin)

FSH	Agonists: Corifollitropin alfa Follicle-stimulating hormone Follitropin alfa Follitropin beta Follitropin epsilon Menotropin (human menopausal gonadotropin) Urofollitropin Varfollitropin alfa NAMs: ADX-61623

Growth factor

See here instead.

Insulin

Antagonists: BMS-754807
S661
S961

Kinase inhibitors: Linsitinib

Kisspeptin

Agonists: Kisspeptin
Kisspeptin-10

Antagonists: Kisspeptin-234

Leptin

Agonists: Leptin
Metreleptin

MCH

MCH₁	Agonists: Melanin concentrating hormone Antagonists: ATC-0065 ATC-0175 GW-803430 NGD-4715 SNAP-7941 SNAP-94847

MCH₂	Agonists: Melanin concentrating hormone

Melanocortin

See here instead.

Neuropeptide FF

Agonists: Neuropeptide AF
Neuropeptide FF
Neuropeptide SF (RFRP-1)
Neuropeptide VF (RFRP-3)

Antagonists: BIBP-3226
RF9

Neuropeptide S

Agonists: Neuropeptide S

Antagonists: ML-154
SHA-68

Neuropeptide Y

Y₁	Agonists: Neuropeptide Y Peptide YY Antagonists: BIBO-3304 BIBP-3226 BVD-10 GR-231118 PD-160170

Y₂	Agonists: 2-Thiouridine 5'-triphosphate Neuropeptide Y Neuropeptide Y (13-36) Peptide YY Peptide YY (3-36) Antagonists: BIIE-0246 JNJ-5207787 SF-11

Y₄	Agonists: GR-231118 Neuropeptide Y Pancreatic polypeptide Peptide YY Antagonists: UR-AK49

Y₅	Agonists: BWX-46 Neuropeptide Y Peptide YY Antagonists: CGP-71683 FMS-586 L-152,804 Lu AA-33810 MK-0557 NTNCB Velneperit (S-2367)

Neurotensin

NTS₁	Agonists: Neurotensin Neuromedin N Antagonists: Meclinertant SR-142948

NTS₂	Agonists: Neurotensin Antagonists: Levocabastine SR-142948

Opioid

See here instead.

Orexin

OX₁	Agonists: Orexin (A, B) Antagonists: ACT-335827 ACT-462206 Almorexant Filorexant Lemborexant SB-334867 SB-408124 SB-649868 Suvorexant TCS-1102

OX₂	Agonists: Orexin (A, B) SB-668875 Antagonists: ACT-335827 ACT-462206 Almorexant EMPA Filorexant JNJ-10397049 MIN-202 (JNJ-42847922) Lemborexant MK-1064 SB-649868 Suvorexant TCS-1102 TCS-OX2-29

Unsorted	Antagonists: Seltorexant

Oxytocin

See here instead.

Prolactin

Antagonists: Δ1–9-G129R-hPRL
Δ1–14-G129R-hPRL
G120K-hGH
G129R-hPRL

PTH

Agonists: Abaloparatide
Parathyroid hormone
Parathyroid hormone-related protein (PTHrP)
Semparatide
Teriparatide

Relaxin

Somatostatin

Agonists: BIM-23052
CH-275
Cortistatin-14
Depreotide
Ilatreotide
L-803,087
L-817,818
Lanreotide
NNC 26-9100
Octreotide
Pasireotide
Pentetreotide
RC-160
Seglitide
Somatostatin (GHIH)
Somatostatin (1-28)
SRIF-14
SRIF-28
TT-232
Vapreotide

Antagonists: BIM-23056
Cyclosomatostatin
CYN-154806
Satoreotide

Tachykinin

NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant

NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant

NK₃	Agonists: Neurokinin B Antagonists: Fezolinetant Osanetant Talnetant

TRH

Agonists: Azetirelin
Fertirelin
Montirelin
Orotirelin
Posatirelin
Protirelin
Rovatirelin
Taltirelin
TRH (TRF)

TSH

Agonists: Thyrotropin alfa
TSH (thyrotropin)

Vasopressin

See here instead.

VIP/PACAP

VIPR₁	Agonists: Peptide: Bay 55-9837 LBT-3393 PACAP VIP

VIPR₂	Agonists: Peptide: LBT-3627 PACAP VIP

PAC₁	Agonists: PACAP PACAP (1-27) PACAP (1-38) Antagonists: PACAP (6-38)

Unsorted	PHI PHM PHV

Others

Endogenous: Adrenomedullin
Apelin
Bombesin
Calcitonin
Carnosine
CART
CLIP
DSIP
Enteroglucagon
Formyl peptide
GALP
GIP
GRP
Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin)
Kininogens
Motilin
Natriuretic peptides (ANP, BNP, CNP, urodilatin)
Nesfatin-1
Neuromedin B
Neuromedin N
Neuromedin S
Neuromedin U
Obestatin
Osteocalcin
Resistin
Secretin
Thymopoietin
Thymosins
Thymulin
Urotensin-II
VGF

Exogenous: Lifitegrast (LFA-1 antagonist)

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