acAb t½ 3.6 d in pooled urothelial PK; shorter than brentuximab (5 d) and tisotumab (4 d) reflecting weight-based dosing in obese urothelial population and higher CL
Payload MMAE is a microtubule (tubulin polymerization) inhibitor. ADCdb in-vitro: enfortumab vedotin IC50 ~1.2-4.7 ng/mL on PC-3 prostate carcinoma and 37.8 ng/mL on T-47D breast carcinoma cells. Clinically FDA-approved Dec 2019 for advanced urothelial cancer.
06
Dosing & regimen
Dosing
RP2D dose
1.25 mg/kg (max 125 mg)
Schedule
D1+D8+D15 Q4W
Route
IV
Fractionated
Yes
n at RP2D
384
Dose basis
TBW
Trial phase
Approved
Dose-OAE available
No
Tox summary basis
RP2D
ADA rate (%)
5 %
07
Pharmacology
Clinical pharmacokinetics
By analyte · FDA label §12.3 + Drugs@FDA clinical-pharmacology reviews
Intact ADC
Free payload
Cmax
28 (±6.1)µg/mL
5.5 (±3.0)ng/mL
AUC
110 (±26)µg·d/mL
85 (±50)ng·d/mL
Tmax
near end of infusion (~0.5)h
~2days
t½
3.6days+1
2.6days+1
CL
0.11L/h+1
2.11L/h+1
Vd
12.8L+1
218L
FDA label §12.3 Drugs@FDA reviewhover a value for dose / population / source · “+N” marks additional reported values
n=384 · pooled single-agent (ophthalmologic-exam-scheduled subset)
EV 1.25 mg/kg
Days 1,8,15 q28d
30%
n=89 · EV-201 Cohort 2
EV 1.25 mg/kg; pembrolizumab 200 mg; sitravatinib (escalation)
EV Days 1,8 q21d
25%
n=4 · Sitravatinib+pembro+EV
EV 1.25 mg/kg; pembrolizumab 200 mg
EV Days 1,8 q21d
25%
n=121 · EV-103
EV 1.25 mg/kg
Days 1,8,15 q28d
24%
n=296 · EV-301
EV 1.25 mg/kg; pembrolizumab 200 mg
EV Days 1,8 q21d
24%
n=440 · EV-302
1.25 mg/kg
Days 1, 8 of 21-day cycle, IV (+ pembrolizumab)
24%
n=440 · EV-302
EV 1.25 mg/kg; pembrolizumab 200 mg
EV Days 1,8 q21d
21%
n=167 · EV-303
EV 1.25 mg/kg
Days 1,8,15 q28d
15.6%
n=45 · EV-202
EV 1.25 mg/kg; pembrolizumab 200 mg; sitravatinib 35 mg QD
EV Days 1,8 q21d
12.5%
n=8 · Sitravatinib+pembro+EV
EV 1.25 mg/kg
Days 1,8,15 q28d
12.5%
n=40 · EV China
EV 1.25 mg/kg
Days 1,8,15 q28d
10.1%
n=296 · EV-301
EV 1.25 mg/kg; pembrolizumab 200 mg
EV Days 1,8 q21d
9.8%
n=41 · EV-202
EV 1.25 mg/kg
Days 1,8,15 q28d
7.2%
n=125 · EV-201
EV 1.25 mg/kg
Days 1,8,15 q28d
2.4%
n=42 · EV-202
EV 1.25 mg/kg
Days 1,8,15 q28d
2.3%
n=43 · EV-202
EV 1.25 mg/kg
Days 1,8,15 q28d
1.1%
n=89 · EV-201
1.25 mg/kg (max 125 mg)
D1+D8+D15 Q4W (monotherapy)
0.7%
n=296 · EV-301
EV 1.25 mg/kg; pembrolizumab 200 mg
EV Days 1,8 q21d
0.2%
n=440 · EV-302
—
10.14%
n=296 · A Study to Evaluate Enfortumab Vedotin Versus (vs) Chemotherapy in Subjects With
—
10%
n=30 · Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatme
—
7.36%
n=326 · A Study to Evaluate Enfortumab Vedotin in Subjects With Locally Advanced or Meta
—
6.25%
n=16 · A Phase 2 Study of Sitravatinib in Combination With PD-(L)1 Checkpoint Inhibitor
—
6.12%
n=49 · Study of Sitravatinib With or Without Other Anticancer Therapies Receiving Clini
—
5.61%
n=214 · EV-201
—
2.8%
n=572 · Perioperative Pembrolizumab (MK-3475) Plus Cystectomy or Perioperative Pembroliz
Per-cohort rates from the per-trial extraction, sorted by dose. Cross-trial comparison is subject to ascertainment / scale differences (see comparability above) — e.g. an early symptom-driven trial can read lower than a later systematic-exam trial at a higher dose.