ADC TOXICITY ATLAS
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LY3076226 (IMC-D11)

Discontinued
IMC-D11; LY-3076226; LY 3076226; anti-FGFR3 ADC IMC-D11; CHEMBL4298017
Sponsor
Eli Lilly (orig. ImClone)
Indication
Advanced/metastatic solid tumours (FGFR3-altered urothelial carcinoma in expansion)
Target family
Receptor tyrosine kinase
RP2D dose
5.0 mg/kg (highest/expansion dose; MTD not reached, no DLTs)
Q3W (Day 1 of each 21-day cycle)Pooled
01
Multi-organ toxicity

Fingerprint & organ drill-down

Also reported
0%severity100%
0
Assessed · clear
true 0%
No data
never assessed
7 adverse-event terms

Ocular

Any-grade
12%
G3+
0%
Pooled
sagittal schematic · -

Tissues shaded by reported adverse-event rate.

Cornea
AE
4%
Express.
-
Limbus
AE
-
Express.
-
Conjunctiva
AE
-
Express.
-
Lens
AE
-
Express.
-
Retina / RPE
AE
-
Express.
-
Dominant tissue
Cornea
Surface subtype
Corneal (off-target)
Reversibility
-
Reported ocular events
Vision blurred12%
n=25
Keratitis4%
n=25
Corneal epithelial microcysts4%
n=25
Dry eye4%
n=25
Photopsia4%
n=25
Retinal pigment epitheliopathy4%
n=25
Eye disorders (any Grade >=3)-
G3+ 0%n=25
02
Construct

Molecular anatomy

Antibody
IgG1
Human
Linker
Cleavable
DAR
Payload
Tubulin inhibitor
Linker structureC13H14N2O4S2
[H]c1nc(SSC([H])([H])C([H])([H])C([H])([H])C(=O)ON2C(=O)C([H])([H])C([H])([H])C2=O)c([H])c([H])c1[H]
Payload structureC38H54ClN3O10S
C[C@@H]1[C@@H]2C[C@]([C@@H](/C=C/C=C(/CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)C[C@@H]([C@]4([C@H]1O4)C)OC(=O)[C@H](C)N(C)C(=O)CCC(C)(C)S)C)\C)OC)(NC(=O)O2)O
03
Antibody

Antibody & Fc engineering

Antibody
IMC-D11
Isotype
IgG1
Origin
Human
Fc modifications
-
Glycoengineering
-
Effector silencing
None
FcγR binding
Retained
C1q binding
Retained
04
Linker & conjugation

Linker chemistry

Linker profile
Linker
SPDB / sulfo-SPDB
Class
Cleavable
Cleavage
Cleavable
Attachment
Lysine
Conjugation
Conventional Lys (SPDB)
Symmetry
Symmetric
DAR (mean)
-
DAR homogeneity
Heterogeneous
Plasma t½
2-7 d
Cleavage trigger
GSH/reductive (disulfide)
Release control
Conditional
Hydrophilicity mask
None
Formula
C13H14N2O4S2
Linker MW
326.399 Da
Linker TPSA
76.57 Ų
Linker xLogP
2.2093
ADCdb linker
LIN0VZYER
In-vitro stability
-
05
Payload

Payload & physicochemistry

Payload profile
Payload
DM4 (free)
Class
Maytansinoid
Mechanism
Tubulin inhibitor
Released catabolite
DM4 and S-methyl-DM4 (S-methyl-DM4 the predominant circulating active catabolite for SPDB-DM4 ADCs)
Mechanistic subtype
Tubulin-maytansinoid
Stereochem / salt
-
Bystander
Yes
PAMPA rank
-
MW
780.4 Da
XLogP3
3.2
logD₇.₄
3
TPSA
157 Ų
pKa
10.3 pKa
Charge pH 7.4
0
H-bond donors
3
H-bond acceptors
11
IC50 (HCEC)
-
Formula
C38H54ClN3O10S
PubChem CID
11686439
ADCdb payload
PAY0GTSVM
Hydrophobicity · logD₇.₄
hydrophilic −2+3+4 lipophilic
06
Dosing & regimen

Dosing

RP2D dose
5.0 mg/kg (highest/expansion dose; MTD not reached, no DLTs)
Schedule
Q3W (Day 1 of each 21-day cycle)
Route
IV
Fractionated
No
n at RP2D
25
Dose basis
TBW
Trial phase
Phase 1
Dose-OAE available
Yes
Tox summary basis
all-doses pooled
07
Ocular & expression

Ocular profile & eye-tissue target expression

Target profile
OAE any-grade
12 %
OAE grade 3+
0 %
OAE data status
reported
Severity (weighted)
3.6
Keratopathy
4 %
Conjunctival
-
Dry eye
4 %
Blurred vision
12 %
Dominant tissue
Cornea
Surface subtype
Corneal (off-target)
Grading scale
CTCAE v4
Reversibility
-
Target expression in eye tissues (HCA detection · HPA bulk)
Cornea (central)
-
Cornea (limbal)
-
Conjunctiva
-
RPE
-
Retina (HPA)
-
Cross-trial comparability · source-verified
Ascertainment: Systematic eye examsScale: CTCAE v4Denominator: RP2D
08
Identity & registry

Identifiers, registry & notes

ADC id
ly3076226
Approval status
Discontinued
Approval year
-
UniProt
P22607
ADCdb ADC
DRG0XBJHU
ADCdb antibody
ANI0OKRWC
ADCdb target
TAR0ZNFNB
Primary source
ClinicalTrials.gov NCT02529553 (posted results) + Invest New Drugs 2021 (PMID 34264412 / DOI 10.1007/s10637-021-01146-x)
Aliases & development codes
IMC-D11; LY-3076226; LY 3076226; anti-FGFR3 ADC IMC-D11; CHEMBL4298017
Notes
LY3076226 (IMC-D11): fully human anti-FGFR3 IgG1 (IMC-D11) conjugated to the maytansinoid DM4 via a reducible disulfide SPDB linker (random Lys / NHS ester). ADCdb ids: ADC DRG0XBJHU, antibody ANI0OKRWC, target TAR0ZNFNB (FGFR3), payload PAY0GTSVM (DM4), linker LIN0VZYER (SPDB, C13H14N2O4S2). The LIN0VZYER physchem (MW 326.399, TPSA 76.57, xLogP 2.2093) is identical to the SPDB entries already in the DB (anetumab-/tusamitamab-ravtansine). Linker labelled 'SPDB / sulfo-SPDB' per DB convention: ADCdb assigns plain SPDB (LIN0VZYER), while some LY3076226 literature describes sulfo-SPDB. DAR is genuinely undisclosed (ADCdb 'Undisclosed'; not in protocol or publication) -> left blank. DM4 payload physchem are the standard shared-payload values (PubChem CID 11686439 Ravtansine; matches existing DB DM4 rows). CLINICAL (NCT02529553, single-arm Phase 1, terminated): 25 treated (Part A escalation 0.2/0.4/0.8/1.6/2.4/3.2/4.0/5.0 mg/kg, n=1,1,1,3,3,4,3,6; Part B expansion at 5.0 mg/kg in FGFR3-altered urothelial carcinoma, n=3). IV Q3W (D1 of 21-day cycle). No DLTs and MTD not reached; 5.0 mg/kg was the top/expansion dose. Only 2 treatment-related Grade 3 events (embolism; decreased platelet count); all other toxicities Grade 1-2. No responses. DENOMINATOR / RP2D NOTE: there is no formal RP2D and per-cohort denominators are tiny (n=1-6), so all percentages and toxicity_rows are computed over the POOLED safety population N=25 (the trial's AE-table denominator: 'all participants who received at least one dose'); these pooled rows are tagged line_context='RP2D' per instruction as the primary analysis cohort, with the 5.0 mg/kg dose-level cohort = n=9 (6 escalation + 3 expansion). n_rp2d set to 25 to match the reported percentages. AE counts re-derived exactly from the raw ClinicalTrials.gov v2 JSON (not the summarizer). Grading per NCI CTCAE v4.0 (confirmed in protocol I7O-MC-JOBA); MedDRA 20.1; AE window up to 33 days post-treatment; events are all-cause TEAEs. OCULAR (why this ADC qualifies): Eye-disorders SOC = vision blurred 3/25 (12%), keratitis 1/25, dry eye 1/25, corneal epithelial microcysts 1/25, photopsia 1/25, retinal pigment epitheliopathy 1/25. oae_any_pct=12.0 (max single PT = vision blurred). ae_corneal_pct=4.0 (max of keratitis/microcysts, each 1/25; union would be 8% across 2 patients). Classified Corneal (off-target) consistent with the DM4 maytansinoid microcystic-keratopathy signature and the DM4 family in the DB; note the SOC also contains a visual (photopsia) and a retinal (retinal pigment epitheliopathy) single-case finding. No ocular event was Grade >=3 (oae_g3plus_pct=0.0, inferred from the publication's complete G3 enumeration). LY3076226-specific ocular reversibility/recovery was not reported -> ae_reversibility left blank. dose_oae_available=True (per-dose-cohort OAE counts available). Zero-valued rows (neutropenia, ILD/pneumonitis, infusion-related reaction) are documented absences from the complete AE listing (frequencyThreshold=0), tier C. payload_name kept as 'DM4 (free)' for DB consistency though ADCdb labels it 'Mertansine DM4'. ADC plasma t1/2 ~2-7 days (publication) recorded in linker_plasma_t_half.