An S1P Receptor Modulator Approved for UC1
Sphingosine 1-phosphate (S1P) signaling plays a role in the pathophysiology of inflammatory
conditions like UC2
S1P
Lymphocyte
Lymphoid
Organ
Efferent
Lymphatic
Vessel
Blood
Vessel
S1P is a signaling molecule that interacts with S1P receptors on lymphocytes.3
Lymphocytes migrate from a low S1P concentration in lymphoid tissue to a high S1P concentration in the circulation and inflamed intestinal tissue.5-8,10
S1P
Receptor
Lymphocyte migration is guided by an S1P
concentration gradient to sites of inflammation.2,4-9
Lymphocyte
S1P
S1P
Receptor
S1P is a signaling molecule that interacts with S1P receptors on lymphocytes.3
Lymphoid
Organ
Efferent
Lymphatic
Vessel
Blood
Vessel
Lymphocytes migrate from a low S1P concentration in lymphoid tissue to a high S1P concentration in the circulation and inflamed intestinal tissue.5-8,10
Lymphocyte migration is guided by an S1P concentration gradient to sites of inflammation.2,4-9
ZEPOSIA is a small
molecule that reversibly
sequesters lymphocytes
in lymphoid tissue1,11,12
The mechanism by which ZEPOSIA exerts therapeutic effects in UC is unknown but may involve the reduction of lymphocyte migration into the intestine.1
Lymphoid
Organ
Efferent
Lymphatic
Vessel
Blood
Vessel
ZEPOSIA
Small Molecule12
ZEPOSIA binds
with high affinity
to S1P receptors
1 and 5.1,11,13a
This blocks the capacity of lymphocytes to egress from lymphoid tissue, reducing the number of lymphocytes in the peripheral circulation.1
ZEPOSIA induces a sustained
internalization of S1P1 receptors.11,13
The mechanism by which ZEPOSIA exerts therapeutic effects in UC is unknown but may involve the reduction of lymphocyte migration into the intestine.1
ZEPOSIA
Small Molecule12
ZEPOSIA binds
with high affinity
to S1P receptors
1 and 5.1,11,13a
Lymphoid
Organ
Efferent
Lymphatic
Vessel
Blood
Vessel
This blocks the capacity of lymphocytes to egress from lymphoid tissue, reducing the number of lymphocytes in the peripheral circulation.1
ZEPOSIA induces a sustained
internalization of S1P1 receptors.11,13
Artist rendering for illustrative purposes
aZEPOSIA has minimal or no activity on SIP receptors 2-4.1
S1P=sphingosine 1-phosphate; UC=ulcerative colitis.