Telisotuzumab vedotin

FDA-approved

Emrelis; Teliso-V; ABBV-399

Target

c-MET (HGFR) · MET

Sponsor

AbbVie

Indication

MET+ NSCLC

Target family

Receptor tyrosine kinase

RP2D dose

1.9 mg/kg

Q2WRP2D

Multi-organ toxicity

Fingerprint & organ drill-down

Also reported

0%severity100%

Assessed · clear

true 0%

No data

never assessed

4 adverse-event terms

Ocular

Any-grade

25%

G3+

1.2%

RP2D

sagittal schematic · Reversible

↳

Tissues shaded by reported adverse-event rate.

Cornea

11%

Express.

26.59%

Limbus

Express.

37.08%

Conjunctiva

Express.

67.14%

Lens

Express.

Retina / RPE

Express.

59.48%

3.6 nTPM

Dominant tissue

Visual

Surface subtype

Visual

Reversibility

Reversible

Reported ocular events

Ocular surface disorders25%

G3+ 1.2%n=168

Vision blurred15%

G3+ 1.2%n=168

Keratitis11%

G3+ 0.6%n=168

Dry eye5%

n=168

Construct

Molecular anatomy

Antibody

IgG1

Humanized

Linker

Cleavable

3.1

DAR

Payload

MMAE

Tubulin inhibitor

Linker structureC28H40N6O7

[H]OC([H])([H])c1c([H])c([H])c(N([H])C(=O)[C@@]([H])(N([H])C(=O)[C@@]([H])(N([H])C(=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N2C(=O)C([H])=C([H])C2=O)C([H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])N([H])C(=O)N([H])[H])c([H])c1[H]

Payload structureC39H67N5O7

CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@H](C)[C@H](C2=CC=CC=C2)O)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC

Antibody

Antibody & Fc engineering

Antibody

ABT-700 (telisotuzumab)

Isotype

IgG1

Origin

Humanized

Fc modifications

None

Glycoengineering

Standard

Effector silencing

None

FcγR binding

Retained

C1q binding

Retained

Linker & conjugation

Linker chemistry

Linker profile

Linker

MC-vc-PAB (vedotin)

Class

Cleavable

Cleavage

Cleavable

Attachment

Cysteine (interchain)

Conjugation

Conventional interchain Cys

Symmetry

Symmetric

DAR (mean)

3.1

DAR homogeneity

Heterogeneous

Plasma t½

3.0 d

Cleavage trigger

Cathepsin B (Val-Cit)

Release control

Conditional

Hydrophilicity mask

None

Formula

C28H40N6O7

Linker MW

572.663 Da

Linker TPSA

200.03 Å²

Linker xLogP

0.6769

ADCdb linker

LIN0SQEDQ

In-vitro stability

Stability note

Mean harmonic t½ 2–4 d for ADC and total antibody (Strickler JCO 2018 Ph1 N=48); within vc-MMAE conventional Cys range

Payload

Payload & physicochemistry

Payload profile

Payload

MMAE

Class

Auristatin

Mechanism

Tubulin inhibitor

Released catabolite

Unconjugated MMAE (monomethyl auristatin E)

Mechanistic subtype

Tubulin-auristatin

Stereochem / salt

Bystander

Yes

PAMPA rank

718 Da

XLogP3

4.1

logD₇.₄

2.7

TPSA

150 Å²

pKa

9.1 pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

IC50 (HCEC)

Formula

C39H67N5O7

PubChem CID

11542188

ADCdb payload

PAY0FSXOW

Hydrophobicity · logD₇.₄

hydrophilic −2+2.7+4 lipophilic

Bioactivity note

ADCdb reports clinical efficacy only (no biochemical IC50/binding for the ADC): ORR ~30.55% in efficacy-evaluable advanced NSCLC combination cohorts; highest observed ORR 71.70% (plus lenalidomide) in a multiple myeloma trial. No payload IC50 or ADC binding-affinity value reporte

Dosing & regimen

Dosing

RP2D dose

1.9 mg/kg

Schedule

Q2W

Route

Fractionated

n at RP2D

168

Dose basis

TBW

Trial phase

Approved

Dose-OAE available

Tox summary basis

RP2D

Ocular & expression

Ocular profile & eye-tissue target expression

Target profile

OAE any-grade

25 %

OAE grade 3+

1.2 %

OAE data status

reported

Severity (weighted)

8.34

Keratopathy

11 %

Conjunctival

Dry eye

5 %

Blurred vision

15 %

Dominant tissue

Visual

Surface subtype

Visual

Grading scale

CTCAE v4

Reversibility

Reversible

Target expression in eye tissues (HCA detection · HPA bulk)

Cornea (central)

26.59 %

Cornea (limbal)

37.08 %

Conjunctiva

67.14 %

RPE

59.48 %

Retina (HPA)

3.6 nTPM

Cross-trial comparability

Ascertainment: Symptom-driven reportingScale: CTCAE v4Denominator: RP2D⚠ OAE rate not directly comparable across trials

Identity & registry

Identifiers, registry & notes

ADC id

telisotuzumab-vedotin

Approval status

FDA-approved

Approval year

2025

UniProt

P08581

ADCdb ADC

DRG0COMTY

ADCdb antibody

ANI0WHSDZ

ADCdb target

TAR0AIJKM

Primary source

EMRELIS PI Section 5.3; LUMINOSITY Camidge JCO 2024

Aliases & development codes

Emrelis; Teliso-V; ABBV-399

Notes

Visual-dominant (blurred 15%) pattern; possible RPE involvement (MET 60% RPE)