ADC TOXICITY ATLAS
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AMG-224

Discontinued
AMG 224; AMG224
Sponsor
Amgen
Indication
Relapsed/refractory multiple myeloma
Target family
TNF receptor superfamily
RP2D dose
3 mg/kg (expansion cohort); MTD = 190 mg flat IV (approx 3 mg/kg)
Every 3 weeks (Q3W)RP2D
01
Multi-organ toxicity

Fingerprint & organ drill-down

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

Ocular

Any-grade
30%
G3+
0%
RP2D
sagittal schematic · Unknown

Tissues shaded by reported adverse-event rate.

Cornea
AE
0%
Express.
0.4%
Limbus
AE
-
Express.
0.6%
Conjunctiva
AE
2.5%
Express.
0.06%
Lens
AE
-
Express.
-
Retina / RPE
AE
-
Express.
0%
0.1 nTPM
Dominant tissue
-
Surface subtype
Unknown
Reversibility
Unknown
Reported ocular events
Treatment-emergent ocular/eye disorders (all PTs)30%
Dry eye10%
Lacrimation increased10%
Vision blurred5%
Conjunctival haemorrhage2.5%
Diplopia2.5%
Eye irritation2.5%
Eye pruritus2.5%
Ocular hyperaemia2.5%
Visual acuity reduced2.5%
Visual impairment2.5%
Vitreous haemorrhage2.5%
Ocular/eye disorders, grade >=3-
G3+ 0%
02
Construct

Molecular anatomy

Antibody
IgG1
Linker
Non-cleavable
DAR
Payload
Microtubule inhibitor (tubulin polymerization inhibitor / anti-mitotic)
Linker structure
structure not applicable
Payload structureC35H48ClN3O10S
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)CCS)C)\C)OC)(NC(=O)O2)O
03
Antibody

Antibody & Fc engineering

Antibody
Anti-human BCMA IgG1 (no INN disclosed)
Isotype
IgG1
Origin
-
Fc modifications
-
Glycoengineering
-
Effector silencing
-
FcγR binding
Retained
C1q binding
Retained
04
Linker & conjugation

Linker chemistry

Linker profile
Linker
MCC (4-[N-maleimidomethyl]cyclohexane-1-carboxylate; SMCC-type)
Class
Thioether (non-cleavable)
Cleavage
Non-cleavable
Attachment
Lysine
Conjugation
Lysine conjugation via non-cleavable MCC/SMCC linker (stochastic; same chemistry as T-DM1)
Symmetry
Symmetric
DAR (mean)
-
DAR homogeneity
-
Plasma t½
-
Cleavage trigger
Non-cleavable (no enzymatic/chemical cleavage site; payload liberated via lysosomal proteolytic degradation of the antibody)
Release control
Unconditional
Hydrophilicity mask
-
Formula
-
Linker MW
-
Linker TPSA
-
Linker xLogP
-
ADCdb linker
-
In-vitro stability
-
05
Payload

Payload & physicochemistry

Payload profile
Payload
DM1 (mertansine / emtansine)
Class
Maytansinoid
Mechanism
Microtubule inhibitor (tubulin polymerization inhibitor / anti-mitotic)
Released catabolite
Lysine-Nepsilon-MCC-DM1 (lys-SMCC-DM1) — inferred by analogy to non-cleavable MCC-DM1 ADCs (e.g., T-DM1)
Mechanistic subtype
Tubulin-maytansinoid
Stereochem / salt
-
Bystander
No
PAMPA rank
-
MW
738.3 Da
XLogP3
2.2
logD₇.₄
-
TPSA
157 Ų
pKa
-
Charge pH 7.4
0
H-bond donors
3
H-bond acceptors
11
IC50 (HCEC)
-
Formula
C35H48ClN3O10S
PubChem CID
11343137
ADCdb payload
PAY0JCIBW
Bioactivity note
Clinical (phase 1, relapsed/refractory multiple myeloma): objective response rate ~23% (2 complete responses, 7 partial responses) in heavily pretreated R/R MM; generally tolerable up to 190 mg every 3 weeks. Source: ADCdb DRG0VFBIW. No discrete payload IC50 or ADC binding KD rep
06
Dosing & regimen

Dosing

RP2D dose
3 mg/kg (expansion cohort); MTD = 190 mg flat IV (approx 3 mg/kg)
Schedule
Every 3 weeks (Q3W)
Route
IV
Fractionated
No
n at RP2D
11 (3 mg/kg expansion cohort: 9 prior anti-CD38, 2 no prior anti-CD38)
Dose basis
TBW
Trial phase
Phase 1
Dose-OAE available
No
Tox summary basis
RP2D
07
Ocular & expression

Ocular profile & eye-tissue target expression

Target profile
OAE any-grade
30 %
OAE grade 3+
0 %
OAE data status
reported
Severity (weighted)
9
Keratopathy
0 %
Conjunctival
2.5 %
Dry eye
10 %
Blurred vision
5 %
Dominant tissue
-
Surface subtype
Unknown
Grading scale
CTCAE (unversioned)
Reversibility
Unknown
Target expression in eye tissues (HCA detection · HPA bulk)
Cornea (central)
0.4 %
Cornea (limbal)
0.6 %
Conjunctiva
0.06 %
RPE
0 %
Retina (HPA)
0.1 nTPM
Cross-trial comparability
Ascertainment: Symptom-driven reportingScale: CTCAE (unversioned)Denominator: RP2D⚠ OAE rate not directly comparable across trials
08
Identity & registry

Identifiers, registry & notes

ADC id
amg-224
Approval status
Discontinued
Approval year
-
UniProt
Q02223
ADCdb ADC
DRG0VFBIW
ADCdb antibody
ANI0IFWTZ
ADCdb target
TAR0KQONX
Primary source
Lee HC, Raje NS, et al. Leukemia 2021;35(1):255-258 (PMID 32317775); NCT02561962 posted results
Aliases & development codes
AMG 224; AMG224
Notes
AMG-224 (Amgen): anti-BCMA (TNFRSF17) human IgG1 conjugated to DM1 (mertansine, maytansinoid microtubule inhibitor) via a NON-CLEAVABLE MCC/SMCC thioether linker through antibody lysine residues (same chemistry as T-DM1). DAR not publicly disclosed (ADCdb, ADC Review, and primary letter all omit it). Phase 1 first-in-human NCT02561962 in relapsed/refractory multiple myeloma: 42 enrolled, 40 in safety analysis set (~21-29 dose-escalation across 7 flat-dose levels 30-250 mg [Doses A-G], 11 in dose-expansion at 3 mg/kg [Dose H]). MTD = 190 mg flat IV Q3W (approximately 3 mg/kg); expansion at 3 mg/kg Q3W. ORR 23% (9/40), median DOR 14.7 months. Program deprioritized July 2017 in favor of Amgen BiTE platform; CT.gov status Completed. QUALIFYING OCULAR DATUM: treatment-emergent ocular AEs grade 1-2 in 30% of patients, no grade >=3, no keratopathy/visual-acuity loss, and crucially NO dose reduction/delay/discontinuation due to ocular toxicity - explicitly contrasted as favorable vs belantamab mafodotin (46% dose-reduced for ocular). One systematic review (PMC12774553) cites 21% (possibly treatment-related-only), reconciled in the toxicity row notes. Specific ocular preferred terms are not disclosed publicly, so ocular_surface_subtype = Unknown (cannot confirm corneal despite maytansinoid class, because keratopathy was explicitly absent). OTHER TOXICITY: thrombocytopenia is the dominant toxicity (treatment-related grade >=3 40%; grade 4 24%); anemia 21%. Neutropenia, fatigue, nausea, and AST increase were also noted among common grade >=3 events but without extractable percentages, so no rows were created for them (blank = not in accessible literature). Peripheral neuropathy not prominent (consistent with non-cleavable DM1 / T-DM1-like profile). SOURCING CAVEAT: the primary publication (Lee et al., Leukemia 2021;35:255-258) is paywalled and PubMed shows 'no abstract'; all efficacy/toxicity figures were obtained via the curated review PMC10137208 (best_source), the BCMA-ADC systematic review PMC12774553, ADC Review drugmap, and the NCT02561962 posted-results module (CT.gov API v2). Composition and dosing are tier B (registry + curated concordant sources); ocular and other toxicity rows are tier C (secondary, primary inaccessible). DM1 physicochemistry is standard shared-payload data from PubChem CID 11343137 (MW 738.3, formula C35H48ClN3O10S, XLogP 2.2, TPSA 157, formal charge 0; non-bystander due to charged lys-MCC-DM1 catabolite). ADCdb did not disclose a linker (LIN) id or any linker physchem for this entry, so the adcdb linker fields are left blank.