Blujepa (gepotidacin): how long were the pivotal tox studies?

13 (13-week rat and dog) (Source: FDA integrated review, p. 66.)

Atlas/Small molecules/Blujepa/Study length

Blujepa: how long were the pivotal tox studies?

gepotidacin · Bacterial topoisomerases (gyrase/topo IV)

Longest pivotal study

13 (13-week rat and dog)

“toxicology studies (repeat-dose studies in rats (up to 13 weeks) and dogs (up to 13 weeks)), genetic toxicology assays (in vitro and in vivo), and reproductive and developmental toxicity in rats and mice.”

✓ VerifiedFDA integrated review, p. 66Source ↗

Pivotal GLP studies

13-week rat and 13-week dog repeat-dose studies

✓ VerifiedFDA integrated review, p. 66Source ↗

Route in tox

Oral (gavage)

“Study #2013N160007 /GSK2140944E: A 13-week Oral (Gavage) Toxicity in Rats Followed by a 28-day Recovery Period”

✓ VerifiedFDA integrated review, p. 126Source ↗

Same question, other small molecules

Accrufer

ferric maltol · Iron replacement

4 (28-day dog)

Adquey

difamilast · PDE4 (topical)

39 (39-week dog and minipig)

Agamree

vamorolone · Glucocorticoid receptor (dissociative)

39 (9-month dog)

Alyftrek

vanzacaftor, tezacaftor and deutivacaftor · CFTR

39 (39-week dog, vanzacaftor)

Anzupgo

delgocitinib · Pan-JAK (topical)

39 (9-month oral dog and dermal minipig)

Aqneursa

levacetylleucine · Neuronal metabolism (proposed)

39 (39-week dog)

Artesunate

artesunate · Plasmodium (antimalarial)

4 (28-day rat and dog)

Attruby

acoramidis · Transthyretin (stabiliser)

39 (39-week dog)

Augtyro

repotrectinib · ROS1/TRK

13 (91-day rat and monkey)

Avmapki Fakzynja Co-pack

avutometinib and defactinib · RAF/MEK clamp; FAK

13 (13-week rat, monkey and dog)

Ayvakit

avapritinib · KIT/PDGFRA

39 (9-month dog)

Azstarys

serdexmethylphenidate and dexmethylphenidate · Dopamine/norepinephrine reuptake

26 (6-month juvenile rabbit)

Balversa

erdafitinib · FGFR1-4

13 (13-week rat and dog)

Barhemsys

amisulpride · Dopamine D2/D3 receptor

4 (28-day rat)

Baxfendy

baxdrostat · Aldosterone synthase (CYP11B2)

39 (9-month monkey)

Beqalzi

sonrotoclax · BCL-2

13 weeks

Brenzavvy

bexagliflozin · SGLT2

39 (39-week monkey)

Brexafemme

ibrexafungerp · Fungal glucan synthase

26 (26-week rat)

Brinsupri

brensocatib · DPP1 (cathepsin C)

39 (9-month dog)

Brukinsa

zanubrutinib · BTK

39 (9-month dog)

Byfavo

remimazolam · GABA-A receptor (benzodiazepine site)

4 (4-week minipig and monkey)

Bylvay

odevixibat · IBAT

39 (39-week dog)

Cabenuva

cabotegravir and rilpivirine · HIV-1 integrase; NNRTI

39 (39-week monkey)

Camzyos

mavacamten · Cardiac myosin

39 (9-month dog)

Caplyta

lumateperone · 5-HT2A / D2 receptor

39 (9-month dog)

Cardamyst

etripamil · L-type calcium channel

26 (6-month monkey)

Cibinqo

abrocitinib · JAK1

39 (9-month monkey)

Cobenfy

xanomeline and trospium · Muscarinic M1/M4 agonist; peripheral antagonist

52 (1-year monkey, xanomeline)

Cosela

trilaciclib · CDK4/6

1 (7-day rat and dog iv)

Crenessity

crinecerfont · CRF1 receptor

52 (12-month dog)

Cypsedo

cipepofol · GABA-A receptor

4 (rat and dog, dosing every other day)

Daybue

trofinetide · IGF-1 tripeptide analogue

39 (39-week dog)

Dayvigo

lemborexant · Orexin OX1/OX2 receptors

39 (9-month monkey)

Defencath

taurolidine and heparin · Antimicrobial catheter lock

2 (14-day rat; not considered pivotal)

Dojolvi

triheptanoin · Anaplerotic energy substrate

39 (9-month juvenile minipig)

Duvyzat

givinostat · Histone deacetylase (class I/II)

39 (39-week monkey)

Egaten

triclabendazole · Fasciola (tubulin)

13 (13-week rat and dog)

Ekterly

sebetralstat · Plasma kallikrein

26 (6-month rat and monkey)

Ensacove

ensartinib · ALK

13 (13-week rat and dog)

Evrysdi

risdiplam · SMN2 splicing

39 (39-week monkey)

Exblifep

cefepime and enmetazobactam · PBPs; beta-lactamase (enmetazobactam)

13 (13-week dog combination study)

Exkivity

mobocertinib · EGFR exon 20 insertion

13 (3-month rat and dog)

Exxua

gepirone · 5-HT1A receptor

52 (12-month dog)

Fabhalta

iptacopan · Complement factor B

39 (39-week dog)

Fetroja

cefiderocol · Penicillin-binding proteins

13 (3-month rat and monkey)

Fexinidazole

fexinidazole · Trypanosoma brucei

4 (28-day rat and dog)

Filspari

sparsentan · Endothelin A / angiotensin II receptors

39 (39-week monkey)

Fotivda

tivozanib · VEGFR1-3

39 (39-week monkey)

Foundayo

orforglipron · GLP-1 receptor (non-peptide)

39 (9-month monkey)

Fruzaqla

fruquintinib · VEGFR1-3

13 (13-week rat and dog GLP studies)

Gavreto

pralsetinib · RET

13 (13-week rat and monkey)

Gemtesa

vibegron · β3-adrenergic receptor

39 (9-month monkey)

Gomekli

mirdametinib · MEK1/2

13 (3-month rat and dog)

Grafapex

treosulfan · DNA alkylation

4 (4-week rat GLP study)

Hernexeos

zongertinib · HER2 (mutant)

13 (13-week rat and dog)

Hyrnuo

sevabertinib · HER2 (mutant)

13 (13-week rat and monkey)

Ibsrela

tenapanor · NHE3

39 (9-month dog)

Ibtrozi

taletrectinib · ROS1

12 (85-day rat and monkey)

Idvynso

doravirine and islatravir · NNRTI; NRTTI

39 (9-month monkey)

Inluriyo

imlunestrant · Estrogen receptor (SERD)

26 (6-month rat)

Inpefa

sotagliflozin · SGLT1/SGLT2

39 (39-week dog)

Inqovi

decitabine and cedazuridine · DNMT (decitabine); cytidine deaminase (cedazuridine)

13 (92-day monkey, 4 cycles)

Inrebic

fedratinib · JAK2

39 (9-month dog)

Iqirvo

elafibranor · PPARα/δ

52 (12-month monkey)

Isturisa

osilodrostat · 11β-hydroxylase (CYP11B1)

39 (39-week dog)

Itovebi

inavolisib · PI3Kα (mutant-selective)

13 (3-month rat and dog)

Jascayd

nerandomilast · PDE4B

39 (39-week minipig and monkey)

Jaypirca

pirtobrutinib · BTK (non-covalent)

13 (3-month rat and dog)

Jesduvroq

daprodustat · HIF prolyl hydroxylase

39 (39-week monkey)

Jideytro

zidesamtinib · ROS1

13 (13-week rat and dog)

Joenja

leniolisib · PI3Kδ

39 (39-week monkey)

Journavx

suzetrigine · NaV1.8

13 (13-week rat and monkey)

Kerendia

finerenone · Mineralocorticoid receptor

39 (9-month dog)

Klisyri

tirbanibulin · Tubulin / Src

4 (28-day oral rat and dog)

Komzifti

ziftomenib · Menin-KMT2A

13 (13-week mouse and dog)

Koselugo

selumetinib · MEK1/2

26 (26-week mouse and monkey)

Krazati

adagrasib · KRAS G12C

13 (13-week rat and dog)

Kygevvi

doxecitine and doxribtimine · Pyrimidine nucleoside replacement (TK2 deficiency)

26 (6-month juvenile rat)

Lampit

nifurtimox · Trypanosoma cruzi

52 (52-week dog)

Lazcluze

lazertinib · EGFR (mutant-selective)

13 (13-week rat and dog)

Leqselvi

deuruxolitinib · JAK1/JAK2

52 (52-week dog)

Lifyorli

relacorilant · Glucocorticoid receptor (antagonist)

39 (39-week monkey)

Litfulo

ritlecitinib · JAK3/TEC kinases

39 (39-week dog)

Livdelzi

seladelpar · PPARδ

52 (52-week monkey)

Livmarli

maralixibat · IBAT (ASBT)

52 (1-year dog)

Livtencity

maribavir · CMV UL97 protein kinase

52 (52-week monkey)

Lumakras

sotorasib · KRAS G12C

13 (3-month rat and dog)

Lupkynis

voclosporin · Calcineurin

39 (39-week monkey)

Lybalvi

olanzapine and samidorphan · D2/5-HT2A; opioid receptors (samidorphan)

39 (9-month dog, samidorphan)

Lynavoy

linerixibat · IBAT

39 (39-week dog)

Lynkuet

elinzanetant · NK1/NK3 receptors

39 (39-week monkey)

Lytgobi

futibatinib · FGFR1-4 (covalent)

13 (13-week rat and dog)

Mayzent

siponimod · S1P1/S1P5 receptor

52 (52-week monkey)

Miebo

perfluorohexyloctane · Tear film evaporation barrier

26 (26-week rabbit ocular)

Miplyffa

arimoclomol · Heat-shock response amplifier

52 (52-week dog)

Modeyso

dordaviprone · DRD2 antagonist / ClpP agonist

13 (13-week rat and dog)

Myqorzo

aficamten · Cardiac myosin

39 (39-week dog)

Nereus

tradipitant · NK1 receptor

26 (6-month rat)

Nexletol

bempedoic acid · ATP citrate lyase

52 (52-week monkey)

Nextstellis

drospirenone and estetrol · Estrogen / progestin receptors

39 (39-week monkey)

Nourianz

istradefylline · Adenosine A2A receptor

52 (52-week dog)

Nubeqa

darolutamide · Androgen receptor

39 (39-week dog)

Nulibry

fosdenopterin · cPMP replacement (MoCD type A)

39 (juvenile dog)

Nurtec ODT

rimegepant · CGRP receptor

39 (9-month monkey)

Nuzolvence

zoliflodacin · Bacterial topoisomerase II

4 (4-week rat and dog)

Ogsiveo

nirogacestat · Gamma secretase

13 (3-month rat and dog)

Ohtuvayre

ensifentrine · PDE3/PDE4

40 (40-week dog)

Ojemda

tovorafenib · RAF (type II pan-RAF)

13 (3-month rat and monkey)

Ojjaara

momelotinib · JAK1/JAK2/ACVR1

39 (39-week dog)

Olinvyk

oliceridine · μ-opioid receptor (G-protein biased)

4 (28-day rat)

Omlonti

omidenepag isopropyl · EP2 receptor

39 (39-week monkey topical ocular)

Ongentys

opicapone · COMT

52 (52-week monkey)

Orgovyx

relugolix · GnRH receptor

39 (39-week monkey)

Orladeyo

berotralstat · Plasma kallikrein

39 (9-month monkey)

Orlynvah

sulopenem etzadroxil and probenecid · Penicillin-binding proteins

4 (1-month rat and monkey)

Orserdu

elacestrant · Estrogen receptor (SERD)

39 (39-week monkey)

Orzeyful

oveporexton · Orexin OX2 receptor agonist

39 (39-week monkey)

Oxbryta

voxelotor · HbS polymerisation

39 (39-week monkey)

Palsonify

paltusotine · Somatostatin receptor 2

39 (9-month dog)

Paxlovid

nirmatrelvir and ritonavir · SARS-CoV-2 Mpro (3CL protease)

4 (1-month rat and monkey)

Pemazyre

pemigatinib · FGFR1-3

13 (3-month rat and monkey)

Piqray

alpelisib · PI3Kα

13 (13-week rat and dog)

Pizensy

lactitol · Osmotic laxative

13 (91-day rat)

Ponvory

ponesimod · S1P1 receptor

52 (52-week dog)

Pretomanid

pretomanid · Mycobacterial cell wall / respiration

39 (9-month monkey)

Pyrukynd

mitapivat · Pyruvate kinase (activator)

39 (9-month monkey)

Qelbree

viloxazine · Norepinephrine reuptake

78 (18-month rat)

Qinlock

ripretinib · KIT/PDGFRA

13 (13-week rat and dog)

Qulipta

atogepant · CGRP receptor

39 (9-month monkey)

Quviviq

daridorexant · Orexin OX1/OX2 receptors

39 (39-week dog)

Rapiblyk

landiolol · β1-adrenergic receptor

4 (4-week rat and dog studies)

Rasonque

daraxonrasib · RAS(ON) multi-selective

13 (13-week mouse and monkey)

Recarbrio

imipenem, cilastatin and relebactam · Beta-lactamase (relebactam)

13 (3-month rat and monkey)

Relyvrio

sodium phenylbutyrate and taurursodiol · ER stress / mitochondrial (proposed)

39 (9-month minipig)

Retevmo

selpercatinib · RET

13 weeks

Revtorpyk

gedatolisib · PI3K/mTOR

13 (3-month rat and dog)

Revuforj

revumenib · Menin-KMT2A

13 (13-week rat and dog)

Reyvow

lasmiditan · 5-HT1F receptor

39 (39-week dog)

Rezdiffra

resmetirom · Thyroid hormone receptor β

39 weeks

Rezlidhia

olutasidenib · IDH1 (mutant)

13 (13-week rat and monkey)

Rezurock

belumosudil · ROCK2

39 (39-week dog)

Rezzayo

rezafungin · Fungal glucan synthase

26 (26-week rat and monkey)

Rhapsido

remibrutinib · BTK

39 (39-week dog)

Rinvoq

upadacitinib · JAK1

39 (39-week dog)

Romvimza

vimseltinib · CSF1R

39 (39-week dog)

Rozlytrek

entrectinib · TRK/ROS1/ALK

13 (13-week rat and dog)

Rukobia

fostemsavir · HIV-1 gp120 (attachment)

39 (9-month dog)

Scemblix

asciminib · BCR-ABL1 (STAMP, myristoyl pocket)

39 (39-week monkey)

Sephience

sepiapterin · Tetrahydrobiopterin precursor

39 (39-week marmoset)

Simtriyo

centanafadine · Triple monoamine reuptake

43 (43-week juvenile dog)

Skyclarys

omaveloxolone · Nrf2 activator

39 (39-week monkey)

Sofdra

sofpironium · Muscarinic receptors (topical)

39 (39-week dermal minipig)

Sohonos

palovarotene · RARγ

39 (39-week dog)

Sotyktu

deucravacitinib · TYK2

39 (9-month monkey)

Sunlenca

lenacapavir · HIV-1 capsid

39 (9-month dog)

Sunosi

solriamfetol · Dopamine/norepinephrine reuptake

52 (12-month dog)

Tabrecta

capmatinib · MET

13 (13-week rat and monkey)

Tavneos

avacopan · C5a receptor (C5aR1)

44 (44-week monkey)

Tazverik

tazemetostat · EZH2

13 (13-week rat and monkey)

Tepmetko

tepotinib · MET

39 (39-week dog)

Trikafta

elexacaftor, tezacaftor and ivacaftor · CFTR

39 (39-week dog, elexacaftor)

Truqap

capivasertib · AKT1-3

39 (9-month dog)

Truseltiq

infigratinib · FGFR1-3

39 (39-week dog)

Tryptyr

acoltremon · TRPM8 agonist

26 (6-month rabbit and dog ocular)

Tryvio

aprocitentan · Endothelin A/B receptors

39 (39-week dog)

Tukysa

tucatinib · HER2

13 weeks

Turalio

pexidartinib · CSF1R

39 (9-month dog)

Ubrelvy

ubrogepant · CGRP receptor

39 (9-month monkey)

Ukoniq

umbralisib · PI3Kδ / CK1ε

39 (39-week dog)

Utebzi

tebipenem pivoxil · Penicillin-binding proteins

4 (28-day GLP rat and monkey; non-GLP studies up to 90 days)

Vafseo

vadadustat · HIF prolyl hydroxylase

39 (9-month dog)

Vanflyta

quizartinib · FLT3

13 (13-week rat, dog and monkey)

Vanrafia

atrasentan · Endothelin A receptor

39 (9-month dog)

Veklury

remdesivir · SARS-CoV-2 RNA polymerase

4 (4-week rat and monkey)

Velsipity

etrasimod · S1P1/S1P4/S1P5 receptors

39 (9-month dog)

Veozah

fezolinetant · Neurokinin-3 receptor

39 (39-week monkey)

Veppanu

vepdegestrant · Estrogen receptor (PROTAC degrader)

39 (9-month dog)

Verquvo

vericiguat · Soluble guanylate cyclase

39 (39-week dog)

Vivjoa

oteseconazole · Fungal CYP51

39 (9-month dog)

Vizz

aceclidine · Muscarinic agonist (miotic)

26 (6-month rabbit ocular)

Vonjo

pacritinib · JAK2/FLT3

39 (39-week dog)

Voquezna

vonoprazan · H+/K+-ATPase (potassium-competitive)

39 (39-week dog)

Voranigo

vorasidenib · IDH1/IDH2

13 (13-week rat and monkey)

Voydeya

danicopan · Complement factor D

39 (39-week dog)

Vtama

tapinarof · Aryl hydrocarbon receptor

39 (9-month minipig)

Vyndaqel

tafamidis · Transthyretin (stabiliser)

39 (39-week dog)

Wakix

pitolisant · Histamine H3 receptor

39 (9-month monkey)

Wayrilz

rilzabrutinib · BTK (reversible covalent)

39 (9-month dog)

Welireg

belzutifan · HIF-2α

13 (3-month rat and dog)

Winlevi

clascoterone · Androgen receptor (topical)

39 (39-week dermal minipig)

Xacduro

sulbactam and durlobactam · PBPs; beta-lactamase (durlobactam)

4 (28-day dog)

Xcopri

cenobamate · Sodium channel / GABA-A

52 (52-week monkey)

Xdemvy

lotilaner · Mite GABA-Cl channel

39 (9-month dog ocular)

Xeglyze

abametapir · Lice metalloproteinases

4 (28-day minipig dermal)

Xenleta

lefamulin · Bacterial ribosome (50S PTC)

13 (13-week IV studies)

Xocova

ensitrelvir · SARS-CoV-2 3CL protease

4 (4-week rat and monkey)

Xolremdi

mavorixafor · CXCR4

39 (39-week dog)

Xpovio

selinexor · XPO1

13 (13-week rat and monkey)

Zavzpret

zavegepant · CGRP receptor

39 (39-week monkey)

Zaynich

cefepime and zidebactam · PBPs; beta-lactam enhancer (zidebactam)

13 (13-week dog)

Zegfrovy

sunvozertinib · EGFR exon 20 insertion

13 (13-week rat and dog)

Zenbexus

iberdomide · Cereblon (CELMoD)

39 (9-month cynomolgus monkey)

Zeposia

ozanimod · S1P1/S1P5 receptor

39 (39-week monkey)

Zepzelca

lurbinectedin · DNA minor groove (transcription)

24 (8-cycle q3w rat and monkey)

Zevtera

ceftobiprole medocaril · Penicillin-binding proteins

13 (13-week rat, marmoset and dog)

Zokinvy

lonafarnib · Farnesyltransferase

52 (1-year monkey)

Ztalmy

ganaxolone · GABA-A receptor (positive modulator)

52 (12-month dog)

Zulresso

brexanolone · GABA-A receptor (positive modulator)

4 weeks

Zurzuvae

zuranolone · GABA-A receptor (positive modulator)

39 (9-month dog)

Zycubo

copper histidinate · Copper replacement (Menkes disease)

13 (13-week juvenile rat)

Summary across all 211 small molecules →