<?xml version="1.0"?>
<ownershipDocument>

    <schemaVersion>X0306</schemaVersion>

    <documentType>4</documentType>

    <periodOfReport>2017-09-19</periodOfReport>

    <issuer>
        <issuerCik>0001069308</issuerCik>
        <issuerName>Acer Therapeutics Inc.</issuerName>
        <issuerTradingSymbol>ACER</issuerTradingSymbol>
    </issuer>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001717553</rptOwnerCik>
            <rptOwnerName>Steiner Robert D</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>222 THIRD STREET</rptOwnerStreet1>
            <rptOwnerStreet2>SUITE #2240</rptOwnerStreet2>
            <rptOwnerCity>CAMBRIDGE</rptOwnerCity>
            <rptOwnerState>MA</rptOwnerState>
            <rptOwnerZipCode>02142</rptOwnerZipCode>
            <rptOwnerStateDescription></rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isOfficer>true</isOfficer>
            <officerTitle>Chief Medical Officer</officerTitle>
        </reportingOwnerRelationship>
    </reportingOwner>

    <derivativeTable>
        <derivativeTransaction>
            <securityTitle>
                <value>Nonqualified Stock Option (right to buy)</value>
            </securityTitle>
            <conversionOrExercisePrice>
                <value>2.55</value>
            </conversionOrExercisePrice>
            <transactionDate>
                <value>2017-09-19</value>
            </transactionDate>
            <transactionCoding>
                <transactionFormType>4</transactionFormType>
                <transactionCode>J</transactionCode>
                <equitySwapInvolved>false</equitySwapInvolved>
                <footnoteId id="F1"/>
            </transactionCoding>
            <transactionAmounts>
                <transactionShares>
                    <value>40000</value>
                </transactionShares>
                <transactionPricePerShare>
                    <footnoteId id="F1"/>
                </transactionPricePerShare>
                <transactionAcquiredDisposedCode>
                    <value>A</value>
                </transactionAcquiredDisposedCode>
            </transactionAmounts>
            <exerciseDate>
                <footnoteId id="F2"/>
            </exerciseDate>
            <expirationDate>
                <value>2026-04-05</value>
            </expirationDate>
            <underlyingSecurity>
                <underlyingSecurityTitle>
                    <value>Common Stock</value>
                </underlyingSecurityTitle>
                <underlyingSecurityShares>
                    <value>40000</value>
                </underlyingSecurityShares>
            </underlyingSecurity>
            <postTransactionAmounts>
                <sharesOwnedFollowingTransaction>
                    <value>40000</value>
                </sharesOwnedFollowingTransaction>
            </postTransactionAmounts>
            <ownershipNature>
                <directOrIndirectOwnership>
                    <value>D</value>
                </directOrIndirectOwnership>
            </ownershipNature>
        </derivativeTransaction>
    </derivativeTable>

    <footnotes>
        <footnote id="F1">Received in connection with the Issuer's business combination (the &quot;Merger&quot;) with what was then known as &quot;Acer Therapeutics Inc.&quot; (&quot;Private Acer&quot;) in accordance with the terms of the Agreement and Plan of Merger and Reorganization dated June 30, 2017 among the Issuer, Opexa Merger Sub, Inc. and Private Acer, in exchange for an option to acquire 40,000 shares of common stock of Private Acer.</footnote>
        <footnote id="F2">Option vests in eight equal quarterly installments beginning on January 1, 2016.</footnote>
    </footnotes>

    <ownerSignature>
        <signatureName>/s/ Daniel S. Clevenger, Attorney-in-Fact for Robert Steiner</signatureName>
        <signatureDate>2017-09-21</signatureDate>
    </ownerSignature>
</ownershipDocument>
