ADC TOXICITY ATLAS
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IMGC-936

Discontinued
IMGC936; IMGC-936; IMGC 936; MGA021-DM21
Sponsor
MacroGenics (co-developed with ImmunoGen/AbbVie)
Indication
Advanced solid tumors (dose-expansion: NSCLC and TNBC)
Target family
Receptor tyrosine kinase
RP2D dose
6.0 mg/kg
IV every 3 weeks (Q3W; Day 1 of 21-day cycle) [Schedule A]; an alternative fractionated Schedule B (Days 1,8,15 of cycles 1-2 then Days 1,8 of a 28-day cycle) was also tested at 2.0 mg/kgRP2D
01
Multi-organ toxicity

Fingerprint & organ drill-down

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

Ocular

Any-grade
77.8%
G3+
-
RP2D
sagittal schematic · Reversible

Tissues shaded by reported adverse-event rate.

Cornea
AE
-
Express.
-
Limbus
AE
-
Express.
-
Conjunctiva
AE
-
Express.
-
Lens
AE
-
Express.
-
Retina / RPE
AE
-
Express.
-
Dominant tissue
Cornea
Surface subtype
Corneal (off-target)
Reversibility
Reversible
Reported ocular events
Vision blurred66.7%
n=6
Keratitis44.4%
n=9
Keratopathy44.4%
n=9
Dry eye38.5%
n=13
Cornea verticillata33.3%
Ocular hyperaemia33.3%
Asthenopia (eye strain)33.3%
Photophobia30.8%
n=13
Punctate keratitis23.1%
n=13
Visual impairment23.1%
n=13
Eye pruritus11.1%
Corneal epithelial microcysts10%
Night blindness10%
Cataract7.7%
n=13
Eye pain7.7%
n=13
Diplopia7.7%
Vitreous floaters7.7%
Lacrimation increased7.7%
Eye irritation7.7%
Foreign body sensation in eyes7.7%
Mycotic endophthalmitis-
02
Construct

Molecular anatomy

Antibody
IgG1
Humanized
Linker
Cleavable
2
DAR
Payload
Microtubule inhibitor (tubulin polymerization inhibitor; antimitotic)
Linker structureC19H28N4O7
C[C@H](NC(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)CCCCCN1C(=O)C=CC1=O)C(=O)O
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)CCCCCS)C)\C)OC)(NC(=O)O2)O
03
Antibody

Antibody & Fc engineering

Antibody
MGA021
Isotype
IgG1
Origin
Humanized
Fc modifications
Engineered cysteine S442C
Glycoengineering
-
Effector silencing
-
FcγR binding
Retained
C1q binding
Retained
04
Linker & conjugation

Linker chemistry

Linker profile
Linker
Mc-Ala-Ala-Ala (DM21-C linker)
Class
Peptide
Cleavage
Cleavable
Attachment
Site-specific (other)
Conjugation
Site-specific (engineered cysteine, S442C)
Symmetry
Site-specific (paired)
DAR (mean)
2
DAR homogeneity
Homogeneous
Plasma t½
-
Cleavage trigger
Protease/peptidase-cleavable (Ala-Ala-Ala tripeptide linker)
Release control
Conditional
Hydrophilicity mask
-
Formula
C19H28N4O7
Linker MW
424.454 Da
Linker TPSA
161.98 Ų
Linker xLogP
-0.9295
ADCdb linker
LIN0TPKXU
In-vitro stability
-
05
Payload

Payload & physicochemistry

Payload profile
Payload
DM21 (linker-payload DM21-C)
Class
Maytansinoid
Mechanism
Microtubule inhibitor (tubulin polymerization inhibitor; antimitotic)
Released catabolite
DM51 (self-immolative thiol catabolite of DM21-C); a maytansinoid microtubule inhibitor
Mechanistic subtype
Tubulin-maytansinoid
Stereochem / salt
-
Bystander
Yes
PAMPA rank
-
MW
780.4 Da
XLogP3
3.3
logD₇.₄
-
TPSA
157 Ų
pKa
-
Charge pH 7.4
0
H-bond donors
3
H-bond acceptors
11
IC50 (HCEC)
-
Formula
C38H54ClN3O10S
PubChem CID
162623843
ADCdb payload
PAY0GFWCQ
Bioactivity note
IMGC936 is a next-generation maytansinoid ADC; the maytansinoid payload inhibits tubulin polymerization/microtubule assembly (anti-mitotic). The protease-released catabolites DM51 and DM50 are membrane-permeable and drive bystander killing. ADCdb assigns the payload therapeutic t
06
Dosing & regimen

Dosing

RP2D dose
6.0 mg/kg
Schedule
IV every 3 weeks (Q3W; Day 1 of 21-day cycle) [Schedule A]; an alternative fractionated Schedule B (Days 1,8,15 of cycles 1-2 then Days 1,8 of a 28-day cycle) was also tested at 2.0 mg/kg
Route
IV
Fractionated
No
n at RP2D
13 (NSCLC dose-expansion at 6.0 mg/kg Q3W); TNBC expansion n=6; 29 total treated at 6.0 mg/kg (10 escalation + 13 NSCLC + 6 TNBC)
Dose basis
TBW
Trial phase
Phase 1/2
Dose-OAE available
Yes
Tox summary basis
RP2D
07
Ocular & expression

Ocular profile & eye-tissue target expression

Target profile
OAE any-grade
77.8 %
OAE grade 3+
-
OAE data status
reported
Severity (weighted)
-
Keratopathy
-
Conjunctival
-
Dry eye
38.5 %
Blurred vision
61.5 %
Dominant tissue
Cornea
Surface subtype
Corneal (off-target)
Grading scale
CTCAE v5
Reversibility
Reversible
Target expression in eye tissues (HCA detection · HPA bulk)
Cornea (central)
-
Cornea (limbal)
-
Conjunctiva
-
RPE
-
Retina (HPA)
-
Cross-trial comparability
Ascertainment: Systematic eye examsScale: CTCAE v5Denominator: RP2D
08
Identity & registry

Identifiers, registry & notes

ADC id
imgc-936
Approval status
Discontinued
Approval year
-
UniProt
Q13443
ADCdb ADC
DRG0RMBUN
ADCdb antibody
ANI0NKMLD
ADCdb target
TAR0DMCMD
Primary source
ClinicalTrials.gov NCT04622774 (posted results 2025-01-15)
Aliases & development codes
IMGC936; IMGC-936; IMGC 936; MGA021-DM21
Notes
PRIMARY-SOURCE UPDATE: Contrary to the wave1 hint ("aggregate % not publicly reported"), ClinicalTrials.gov posted FULL results for NCT04622774 on 2025-01-15. Study = Phase 1 FIH (of Phase 1/2), 56 patients: Schedule A dose escalation 0.5-7.0 mg/kg IV Q3W (21-day cycle, DLT window 21d), a fractionated Schedule B (2.0 mg/kg Days 1,8,15 then 3.0 mg/kg Days 1,8 of 28-day cycle, n=3), and dose expansion at RP2D 6.0 mg/kg Q3W in NSCLC (n=13) and TNBC (n=6). RP2D = 6.0 mg/kg Q3W (protocol explicitly conducts expansion "at the RP2D"; CT.gov shows expansion at 6.0 mg/kg). I tagged the NSCLC expansion (largest single RP2D cohort, n=13) as the primary RP2D ocular line. OCULAR (why this ADC qualifies): Dominant, dose-dependent corneal/ocular-surface toxicity (classic off-target maytansinoid). Vision blurred rose 33.3% (1.0 mg/kg) -> 60% (6.0) -> 77.8% (7.0). At RP2D 6.0 mg/kg (NSCLC n=13): vision blurred 61.5%, dry eye 38.5%, photophobia 30.8%, punctate keratitis 23.1%, visual impairment 23.1%, keratitis 15.4%, keratopathy 15.4%. Other corneal PTs across cohorts: corneal epithelial microcysts and cornea verticillata (Schedule B). Sponsor (MGC028 paper PMID 41166694) states IMGC936 was "affected by dose-limiting ocular adverse events, including blurred vision and keratopathy... no other prominent safety signals." oae_g3plus_pct left blank: CT.gov posted AE module is all-grade (not CTCAE-graded) and no ocular event was serious; grade-specific ocular incidence is not publicly disclosed. CLEAN-ELSEWHERE PROFILE (documented absences via CT.gov threshold-0 AE table, all 56 pts): NO neutropenia/neutrophil count decreased anywhere; peripheral neuropathy only 2 isolated low-dose cases (none at RP2D). I recorded these as pct=0 RP2D rows because the threshold-0 table documents the absence (corroborated by the "no other prominent safety signals" statement) — not an imputed 0. PAYLOAD DISCREPANCY FLAG: ADCdb lists ADC synonym "AEX6003 (S442C)-DGN549" yet its payload field is "DM21-C" with a "Microtubule" mechanism. DGN549 is an unrelated ImmunoGen IGN (DNA-alkylating) payload; ALL authoritative sources (MacroGenics, AACR 2019 abstr 3898/538, AACR 2021 abstr 1841, the protocol's "Maytansinoids are known to cause ocular toxicity," and the MGC028 paper) confirm IMGC936's payload is DM21, a next-generation maytansinoid (microtubule inhibitor), DAR 2.0, site-specifically conjugated via engineered cysteine S442C with a cleavable Mc-Ala-Ala-Ala tripeptide linker; major catabolite DM51. Treated the DGN549 token as a likely ADCdb data error. PAYLOAD PHYSCHEM: DM21 is proprietary and not in PubChem; exact MW/xLogP/logD/TPSA/pKa/charge are not publicly disclosed, so left blank (DM21 is NOT one of the standard shared payloads, so DM1/DM4 values were deliberately NOT substituted). Bystander = yes (designed for efficient hydrophobic catabolite release vs DM4). SOURCE CHECK: Of the wave1 best_source list, the Oncologist 2024 ADC ocular review (academic.oup.com/oncolo/article/29/11/e1435) was fetched and verified to NOT mention IMGC936; the authoritative quantitative data come from CT.gov posted results (used here). Antibody isotype not disclosed by ADCdb (left blank); antibody is a humanized mAb (MGA021) bearing an engineered S442C cysteine in CH3 for site-specific conjugation. Development discontinued 2024 (MacroGenics/AbbVie) for not meeting pre-set safety/efficacy benchmarks (ocular toxicity constrained the therapeutic window); follow-on ADAM9 ADC MGC028 switched to an exatecan topoisomerase-1 payload specifically to avoid the maytansinoid ocular toxicity. Note: ADAM9 is expressed in cornea/retina (ADAM9 loss-of-function causes cone-rod dystrophy), so a minor on-target corneal contribution cannot be fully excluded, but the toxicity pattern matches generic off-target maytansinoid corneal epithelial toxicity, hence ocular_surface_subtype = Corneal (off-target). All toxicity_rows are all-cause TEAEs (CT.gov), all-grade, tier B (primary posted results). Saved local copies: protocol text /tmp/imgc936_prot.txt; CT.gov JSON /tmp/imgc936.json.